Ponatinib, also known as AP24534 is an oral drug for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome–positive (Ph+) acute lymphoblastic leukemia (ALL). It is a multi-targeted tyrosine-kinase inhibitor. Some forms of CML, those that have the T315I mutation, are resistant to current therapies such as imatinib. Ponatinib has been designed to be effective against these types of tumors. Ponatinib was approved in 2012.

Carubicin HCl is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.

Doxorubicin free base, also called doxorubicin, is an anthracycline antibiotic with antineoplastic activity. Approved API for cancer therapeutic use is doxorubicin HCl. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the h

Ceritinib, also known as LDK-378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.

Abiraterone acetate is an FDA approved drug, and is an orally active acetate ester of the steroidal compound abiraterone with antiandrogen activity. Abiraterone acetate was approved by the U.S. Food and Drug Administration (FDA) in April 2011. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. FDA Approval this drug in May 2011.

GS-9219 is a prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations.

Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Quisinostat, also known as JNJ-26481585, is an orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Compared to some first generation HDAC inhibitors, JNJ-26481585 may induce superior HSP70 upregulation and bcl-2 downregulation.

Nemorubicin, also known as PNU152243A, is a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail. Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases.

Idronoxil, also known as Phenoxodiol, is a synthetic flavonoid derivative. Phenoxodiol activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death.

Photochlor, also known as HTTP, is a lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration.

Pixantrone is a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity. Pixantrone is a potentially more effective, less cardiotoxic alternative to doxorubicin for patients with aggressive non-Hodgkin lymphoma (aNHL).

SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

VAL-083 is a bi-functional alkylating agent, with potential antineoplastic activity. Upon administration, VAL-083 crosses the blood brain barrier (BBB) and appears to be selective for tumor cells. This agent alkylates and crosslinks DNA which ultimately leads to a reduction in cancer cell proliferation. In addition, VAL-083 does not show cross-resistance to other conventional chemotherapeutic agents and has a long half-life in the brain.

Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is now in a Phase II clinical trial for the treatment of pediatric neuroblastoma and medulloblastoma. Nifurtimox decreased cell viability in a concentration-dependent manner. Nifurtimox also suppressed basal and TrkB-mediated Akt phosphorylation, and the cytotoxicity of nifurtimox was attenuated by a tyrosine hydroxylase inhibitor (alpha-methyl-tyrosine). Nifurtimox killed catecholaminergic, but not cholinergic, autonomic neurons in culture. In vivo xenograft models showed inhibition of tumor growth with a histologic decrease in proliferation and increase in apoptosis. These results suggest that nifurtimox induces cell death in neuroblastoma . Therefore, further studies are warranted to develop nifurtimox as a promising new treatment for neuroblastoma.

Dilmapimod, also known as SB-681323 and GW-681323 , is p38 MAPK inhibitor. SB-681323 inhibited the p38 MAPK pathway to a greater degree than prednisolone did. SB-681323 inhibited TNF-alpha production. SB-681323 is a potent p38 MAPK inhibitor that potentia

Supinoxin, also known as RX-5902, is orally bioavailable small molecule inhibitor of phosphorylated-p68 RNA helicase (P-p68), with potential anti-proliferative and antineoplastic activity. Upon oral administration, P-p68 inhibitor RX-5902 may both inhibit the activity of the anti-apoptotic B-cell lymphoma 2 (Bcl-2) protein and facilitate the induction of cyclin-dependent kinase inhibitor 1 (p21). This may prevent G2/M cell cycle progression and lead to growth inhibition in tumor cells. P-p68 is overexpressed in various types of solid tumors but absent in normal tissues, and plays a role in tumor progression and metastasis.

Sacubitrilat, also known as LBQ-657, is endopeptidase inhibitor. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides that work mainly by reducing blood volume.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) with IC50 values of 8nM and 8.2nM for I-IP-10 and I-ITAC, respectively. AMG 487 prevents the chemokines I-IP-10 and I-ITAC from binding to CXCR3. In the cellular assays, AMG 487 inhibits CXCR3-mediated cell migration with IC50 values of 8nM, 15nM and 36nM for I-IP-10, I-ITAC and MIG, respectively.

Mafodotin, also known as mc-MMAF and SGD-1269 or Maleimidocaproyl monomethylauristatin F, is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful a

Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

Maytansinoid DM4, a chemical derivative of maytansine, is a potent and selective cytotoxic agent with promising anticancer properties. Anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. Maytansin

ONC206 is a chemical analogue of ONC201. ONC206 is a benzyl-flurobenzyl imipridone that has highly potent activity in preclinical models of difficult-to-treat neuroendocrine tumors and sarcomas. ONC206 acts as a selective antagonist of DRD2 at nanomolar concentrations and has broad-spectrum anti-tumor activity. ONC206 may address tumor types where the properties of ONC201 do not permit for complete therapeutic engagement in vivo.

ATN-161 is a small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration. Note: The Catalog number of ATN-161 TFA salt was changed from 200350B to 206976.

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.

CCS-1477 is a potent and selective p300/CBP bromodomain inhibitor, is targeted & differentiated from BET inhibitors in prostate cancer cell lines in vitro. Combination of CCS1477 & JQ1 resulted in a highly synergistic inhibitory effect on proliferation in normal 22Rv1 cells. Global gene expression analysis revealed significantly fewer altered genes after CCS1477 (27 up, 119 down) compared to JQ1 (196 up, 655 down).

Tipranavir is a nonpeptidic protease inhibitor. Tipranavir has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and it recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations. Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. Like lopinavir and atazanavir, it is very potent and is effective in salvage therapy for patients with some drug resistance.

Tazobactam inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups. It is commonly used as its sodium salt, tazobactam sodium. Tazobactam is combined with the extended spectrum β-lactam antibiotic piperacillin in the drug piperacillin/tazobactam, one of the preferred antibiotic treatments for nosocomial pneumonia caused by Pseudomonas aeruginosa.[medical citation needed] Tazobactam broadens the spectrum of piperacillin by making it effective against organisms that express β-lactamase and would normally degrade piperacillin. Tazobactam is derived from the penicillin nucleus and is a penicillinic acid sulfone.

Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1.

Alprenolol HCl, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non-selective beta blocker as well as 5-HT1A receptor antagonist, used in the treatment of angina pectoris. It is no longer marketed by AstraZeneca, but may still be available from other pharmaceutical companies or generically.

Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In Italy, it is also used as a treatment for dysthymia. It was introduced by Sanofi-Aventis in the 1990s. Its patent had expired by 2008 and hence generic formulations are now available.Amisulpride function primarily as a D2 and D3 receptor antagonist. It has high affinity for these receptors with dissociation constants of 2.2 nM and 2.4 nM, respectively. Although standard doses used to treat psychosis inhibit dopaminergic neurotransmission, low doses preferentially block inhibitory pre-synaptic autoreceptors.

Amlexanox, also known as AA-673 and CHX 3673, is an anti-inflammatory antiallergic immunomodulator used to treat recurrent aphthous ulcers (canker sores), and (in Japan) several inflammatory conditions. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Balsalazide Disodium is the disodium salt form of balsalazide, an aminosalicylate and oral prodrug that is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Mesalazine acts locally on the mucosa of the colon where it diminishes inflammation by blocking the production of arachidonic acid metabolites and other inflammatory agents. Balsalazide disodium is used to treat chronic inflammatory bowel disease.

Butoconazole is an imidazole antifungal used in gynecology. It is administered as a vaginal cream.

Cefotetan Sodium, also known as ICI-156834 and YM-09330, is a second-generation cephalosporin, cephamycin antibiotic that is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative bacteria. Cefotetan binds to penicillin-binding proteins and disrupts the cell wall synthesis.

Danazol is a derivative of the synthetic steroid ethisterone that suppresses the production of gonadotropins and has some weak androgenic effects. Before becoming available as a generic drug, danazol was marketed as Danocrine in the United States. It was approved by the US Food and Drug Administration (FDA) as the first drug to specifically treat endometriosis in the early 1970s. Although effective for endometriosis, its use is limited by its masculinizing side-effects. Its role as a treatment for endometriosis has been largely replaced by the GnRH agonists.

Dicoumarol (INN) or dicumarol (USAN) is a naturally occurring anticoagulant that functions as a functional vitamin K depleter (similar to warfarin, a drug that dicoumarol inspired). It is also used in biochemical experiments as an inhibitor of reductases. Like all 4-hydroxycoumarin drugs it is a competitive inhibitor of vitamin K epoxide reductase, an enzyme that recycles vitamin K, thus causing depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes. These compounds are not antagonists of Vitamin K directly—as they are in pharmaceutical uses—but rather promote depletion of vitamin K in bodily tissues allowing vitamin K's mechanism of action as a potent medication for dicoumarol toxicity. The mechanism of action of Vitamin K along with the toxicity of dicoumarol are measured with the prothrombin time (PT) blood test. (Source: https://en.wikipedia.org/wiki/Dicoumarol).

Dydrogesterone is a synthetic progestin. Dydrogesterone alone or in combination with estrogen to endothelial cells results in neutral effects on NO synthesis and on the activity and expression of eNOS. Unlike many other progestational compounds, dydrogesterone produces no increase in temperature and does not inhibit ovulation.

Eptifibatide, also co-promoted by Schering-Plough/Essex, is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). It belongs to the class of the arginin-glycin-aspartat-mimetics and reversibly binds to platelets. Eptifibatide has a short half-life. The drug is the third inhibitor of GPIIb/IIIa that has found broad acceptance after the specific antibody abciximab and the non-peptide tirofiban entered the global market.

Finasteride is a medication used for the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB). It is a type II and type III 5α-reductase inhibitor; 5α-reductase, an enzyme, converts testosterone to dihydrotestosterone (DHT).

Methacholine chloride is used to constrict airway smooth muscle and to assess bronchial reactivity. Methacholine chloride is a cholinergic agonist and parasympathomimetic bronchoconstrictor. A metabolically stable analog of acetylcholine, it is a muscarin

Metipranolol is a non-selective beta blocker used in eye drops to treat glaucoma. It is rapidly metabolized into desacetylmetipranolol.

Mianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic (anti-anxiety), hypnotic (sedating), antiemetic (nausea and vomiting-attenuating), orexigenic (appetite-stimulating), and antihistamine effects.

Oxiconazole is an antifungal medication typically administered in a cream or lotion to treat skin infections, such as athlete's foot, jock itch and ringworm. It can also be prescribed to treat the skin rash known as tinea versicolor, caused by systemic yeast overgrowth (Candida spp.).

Pindolol is a moderately lipophilic beta blocker. Pindolol is a SR-1A/SR-1B antagonist with similar affinity for each subtype. Pindolol acts as a partial agonist at mouse and human β3-AR (β3-adrenoceptors). Pindolol is an inhibitor of β1-AR.

Prednisolone sodium phosphate is a water soluble form of prednisolone, a glucocorticoid. It is used to treat a variety of inflammatory and autoimmune conditions and some cancers. It is the active metabolite of the drug prednisone and is used especially in patients with liver failure, as these individuals are unable to metabolize prednisone into active prednisolone.

Mianserin hydrochloride is a tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.

Zidebactam, also known as WCK-5107, is a Beta lactamase inhibitor. Zidebactam is a novel Inhibitor of PBP2 Showing Potent "β-Lactam Enhancer" Activity against Pseudomonas aeruginosa, Including Multidrug-Resistant Metallo-β-Lactamase-Producing High-Risk Clones. Zidebactam demonstrated specific high-affinity binding to PBP2 of A. baumannii (0.01 μg/ml for both of the compounds). The MIC of zidebactam was >1,024 μg/ml for wild-type and multidrug-resistant Acinetobacter strains. Zidebactam is a PBP2 inhibitor that show a potent β-lactam enhancer effect against A. baumannii, including a multidrug-resistant OXA-23-producing ST2 international clone.

Lascufloxacin, also known as KRP-AM-1977, is a potent antibacterial drug candidate. Lascufloxacin showed a broad spectrum of activity against various clinical isolates. Especially, lascufloxacin showed the most potent activity against gram-positive bacteria among the quinolones tested. Furthermore, lascufloxacin showed incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin showed potent inhibitory activity against both wild-type and mutated target enzymes. Lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains.

Cimicoxib, aslo known as UR-8880, is a non-steroidal anti-inflammatory drug (NSAID) used in veterinary medicine to treat dogs for pain and inflammation associated with osteoarthritis and for the management of pain and inflammation associated with surgery. It acts as a COX-2 inhibitor.

Emeramide, also known as NBMI, BDTH2 or N,N'-Bis(2-mercaptoethyl)isophthalamide, is a mercury/heavy metal chelator. Emeramide molecule consists of two thiol groups and linked via a pair of amide groups. NBMI can be used to chelate heavy metals like lead, cadmium, copper, manganese, zinc, iron, and mercury from ground water, coal tailings, gold ore, waste water of battery-recycling plants, and contaminated soil.

Glycerol phenylbutyrate, also known as HPN-100, is under trials in the treatment of certain inborn urea cycle disorders. The medication works by preventing the harmful buildup of ammonia in the body. Ammonia is a neurotoxic agent that is primarily generated in the intestine and detoxified in the liver. Toxic increases in systemic ammonia levels predominantly result from an inherited or acquired impairment in hepatic detoxification and lead to potentially life-threatening neuropsychiatric symptoms.

Eprotirome, also known as KB-2115, is a liver-selective thyroid hormone receptor agonist that has been shown to lower plasma LDL cholesterol concentrations in previous phase 1 and 2 studies of patients with dyslipidaemia. KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans.

Velneperit, also known as S-2367, is potent and selective neuropeptide Y Y5-receptor antagonist under evaluating for treatment of obesity.

Lubiprostone, also known as RU-0211, is a medication used in the management of chronic idiopathic constipation, predominantly irritable bowel syndrome-associated constipation in women and opioid-induced constipation. It was initially approved by the U.S. Food and Drug Administration (FDA) in 2006. Lubiprostone is a bicyclic fatty acid derived from prostaglandin E1 that acts by specifically activating ClC-2 chloride channels on the apical aspect of gastrointestinal epithelial cells, producing a chloride-rich fluid secretion. These secretions soften the stool, increase motility, and promote spontaneous bowel movements (SBM).

Sugammadex is an agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). Sugammadex is a modified γ-cyclodextrin, with a lipophilic core and a hydrophilic periphery. This gamma cyclodextrin has been modified from its natural state by placing eight carboxyl thio ether groups at the sixth carbon positions. These extensions extend the cavity size allowing greater encapsulation of the rocuronium molecule. These negatively charged extensions electrostatically bind to the quaternary nitrogen of the target as well as contribute to the aqueous nature of the cyclodextrin.

Sugammadex sodium is an agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). Sugammadex is a modified γ-cyclodextrin, with a lipophilic core and a hydrophilic periphery. This gamma cyclodextrin has been modified from its natural state by placing eight carboxyl thio ether groups at the sixth carbon positions. These extensions extend the cavity size allowing greater encapsulation of the rocuronium molecule.

Alarelin is a potent LH-RH agonist in rats and mice. Alarelin reversibly delays sexual maturation in rats, stimulates spawning activity in fish. GnRH ( gonadotropin-releasing hormone, Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2), which is also referred as LHRH (luteinizing hormone-releasing hormone) or gonadorelin, is crucial for mammalian reproduction and is released from hypothalamic neurons. It is responsible for the secretion of gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), from the pituitary glands.

Argpressin is the predominant form of mammalian antidiuretic hormone. Argpressin is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked CYSTEINES at residues of 1 and 6. Arg-vasopressin is used to treat diabetes insipidus or to improve vasomotor tone and blood pressure.

Gonadorelin is a decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stim. Gonadorelin has been shown to have gonadotropin-releasing effects upon the anterior pituitary.

Mozavaptan, also known as OPC 31260, is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors.

Ivermectin is a medication that is effective against many types of parasites. It is used to treat head lice, scabies, river blindness, strongyloidiasis, and lymphatic filariasis, among others. Ivermectin and other avermectins (insecticides most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission. Ivermectin is a mixture of mostly avermectin H2B1a (CAS# 71827-03-7) with some avermectin H2B1b (CAS# 70209-81-3), which are macrolides from STREPTOMYCES avermitilis.

Pamabrom is a diuretic product included in retail drugs available in over-the-counter medications. The active diuretic ingredient in pamabrom is 8-bromotheophylline. Pamabrom is used in combination with acetaminophen (paracetamol) for various conditions such as back pain and menstrual relief. The acetaminophen helps reduce menstrual pains and the pamabrom reduces associated bloating.

Bretazenil, also known as Ro 16-6028, is GABA A receptor agonist potentially for the treatment of anxiety disorders. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes.

Pimavanserin, also known as ACP-103, is a non-dopaminergic atypical antipsychotic for the treatment of Parkinson's disease psychosis and schizophrenia. Pimavanserin has a unique mechanism of action relative to other antipsychotics, behaving as a selective inverse agonist of the serotonin 5-HT2A receptor, with 40-fold selectivity for this site over the 5-HT2C receptor and no significant affinity or activity at the 5-HT2B receptor or dopamine receptors. It was approved by the FDA to treat hallucinations and delusions associated with psychosis experienced by some people with Parkinson's disease on April 29, 2016.

Ipamorelin, also known as NNC-26-0161, is a a ghrelin mimetic. Ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. Ipamorelin may ameliorate the symptoms in patients with POI. Ipamorelin accelerates gastric emptying in a rodent model of postoperative ileus through the stimulation of gastric contractility by activating a ghrelin receptor-mediated mechanism involving cholinergic excitatory neurons.

Ipriflavone, also known as Yambolap and FL-113, is an osteoclast inhibitor and is effective for enhancing osteoblastic bone formation.

Indocyanine Green, also known as Cardio-Green and Fox, is a tricarbocyanine dye that is used diagnostically in liver function tests and to determine blood volume and cardiac output.

Floctafenine, also known as R-4318 and Idarac, is a cyclooxygenase inhibitor that inhibits prostaglandin synthesis.

Colfosceril Palmitate, also known as 129Y-83 and DPPC, is the primary surface-active agent of natural lung surfactant and the major constituent of exogenous surface replacement preparations. Colfosceril Palmitate is used for the prophylaxis and treatment of neonatal respiratory distress syndrome.

Auranofin, also known as Ridaura and SKF-39162, is an oral chrysotherapeutic agent for the treatment of rheumatoid arthritis. Auranofin's exact mechanism of action is unknown, but it is believed to act via immunological mechanisms and alteration of lysosomal enzyme activity. Auranofin's efficacy is slightly less than that of injected gold salts, but it is better tolerated, and side effects which occur are potentially less serious.

Sulopenem, also known as CP-70429, is a potent beta-lactamase inhibitor.Sulopenem showed potent antibacterial activity against gram-positive and gram-negative bacteria except Pseudomonas aeruginosa and Xanthomonas maltophilia. CP-70,429 was stable to various types of beta-lactamases except for the enzyme from X. maltophilia and was 16- to 128-fold more active than the other compounds against beta-lactamase-producing strains of Enterobacter cloacae and Citrobacter freundii.

Isoindigotin is a potential antileukemic agent.

Nicotinamide riboside, also known as NR and SRT647, is a pyridine-nucleoside form of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide or NAD+. NR blocks degeneration of surgically severed dorsal root ganglion neurons ex vivo and protects against noise-induced hearing loss in living mice. Nicotinamide riboside prevents muscle, neural and melanocyte stem cell senescence. Increased muscular regeneration in mice has been observed after treatment with nicotinamide riboside, leading to speculation that it might improve regeneration of organs such as the liver, kidney, and heart. Nicotinamide riboside also lowers blood glucose and fatty liver in prediabetic and type 2 diabetic models while preventing the development of diabetic peripheral neuropathy. Note: Nicotinamide Riboside chloride is a α/β mixture

Pseudouridine (abbreviated by the Greek letter psi- Ψ) is an isomer of the nucleoside uridine in which the uracil is attached via a carbon-carbon instead of a nitrogen-carbon glycosidic bond. It is the most prevalent of the over one hundred different modified nucleosides found in RNA. Ψ is found in all species and in many classes of RNA. Ψ is formed by enzymes called Ψ synthases, which post-transcriptionally isomerize specific uridine residues in RNA in a process termed pseudouridylation.

Sacubitril, also known as AHU377, is angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the e

Azeliragon 2HCl (also known as TTP488 2HCl and PF-04494700 2HCl) is a potent and orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.

Synephrine, or, more specifically, p-synephrine, is an alkaloid, occurring naturally in some plants and animals, and also in approved drugs products as its m-substituted analog known as neo-synephrine. p-Synephrine and m-synephrine are known for their longer acting adrenergic effects compared to norepinephrine. This substance is present at very low concentrations in common foodstuffs such as orange juice and other orange (Citrus species) products, both of the "sweet" and "bitter" variety.

Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27. It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone I.V. Injection 10 mg" and "Serotone Tablets 10 mg".

Pritelivir, also known as AIC-316 and BAY 57-1293, is a potent helicase primase inhibitor. BAY 57-1293 inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations.

Cenicriviroc, also known as TAK-652 and TBR-652, is an experimental drug candidate for the treatment of HIV infection. It is being developed by Takeda Pharmaceutical and Tobira Therapeutics. Cenicriviroc is an inhibitor of CCR2 and CCR5 receptors, allowi

Gramicidin is a combination of six different antimicrobial polypeptides (from Bacillus aneurinolyticus (Bacillus brevis)).

Parbendazole is an anthelmintic drug. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin and exhibits a broad-spectrum anthelmintic activity.

Nicotinamide Mononucleotide, also known as ("NMN" and "β-NMN") is a nucleotide derived from ribose and nicotinamide Like nicotinamide riboside, NMN is a derivative of niacin, and humans have enzymes that can use NMN to generate nicotinamide adenine dinuc

Matrixyl, also known as Palmitoyl pentapeptide-4 (palmitoyl pentapeptide-3 before 2006) is a matrikine used in anti-wrinkle cosmetics. It was launched in 2000 as an active ingredient for the personal care industry under the trade name Matrixyl by the French cosmetic active ingredient manufacturer Sederma SAS.

Argireline, also known as Acetyl Hexapeptide-3, is a newer ingredient in skincare, ideal for maturing skin and diminishing the appearance of wrinkles. Argireline is the brand name of Acetyl Hexapeptide-8, a molecule formed principally of 6 amino acids (which in a row are called a peptide). It is synthetically produced in a lab, but there are no indications of any degree of toxicity and it is one of our favorite compounds for maturing skin.

Elexacaftor, also known as VX-445 and WHO 11180, is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function in patients with cystic fibrosis when administered with tezacaftor and ivacaftor (VX-445–tezacaftor–ivacaftor).

Brassinazole is an inhibitor of brassinosteroid biosynthesis that has been developed in order to probe the myriad functions of brassinosteroids.

Afamelanotide, also known as CUV1647, is a Melanocortin receptor agonist. Afamelanotide is a synthetic peptide and analogue of α-melanocyte stimulating hormone used to prevent skin damage from the sun in people with erythropoietic protoporphyria .It is under development in other skin disorders in several jurisdictions. It causes skin to turn darker by causing the skin to make more melanin.

Lasmiditan, also known as COL-144 and LY573144, is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (K1=2.21 μM) without vasoconstrictor activity that seemed effective when given as an intravenous infusion in a proof-of-concept migraine study. Lasmiditan showed efficacy in its primary endpoint, with a 2-hour placebo-subtracted headache response of 28.8%, though with frequent reports of dizziness, paresthesias, and vertigo.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Siponimod, also known as BAF-312, is a a potent and orally selective S1P Receptor Modulator with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively. Development of sphingosine-1-phosphate receptor 1 (S1P1) modulators to dampen inflammation and its sequelae is becoming increasingly promising for treating medical conditions characterized by significant immunopathology.

Fatostatin A is a Cell permeable inhibitor of SREBP activation. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma.

Eyeseryl, also known as Acetyl Tetrapeptide-5, humectant or hydroscopic moisturizer which helps reduce eye puffiness, improve skin elasticity as well as overall smoothness.

B355252 is a neuroprotective agent that potentiates nerve growth factor (NGF)-induced neurite outgrowth and protects against cell death caused by glutamate-evoked oxidative stress.

Rhodamine 123 is a chemical compound and a dye.

Pyrinuron is a chemical compound formerly used as a rodenticide. Pyrinuron is an inhibitor of NAMPT and NMNAT2.

Zinc Pyrithione is a dimer of two pyrithione molecules bound by zinc. It is commonly found as an ingredient of commercial anti-dandruff shampoos. This products acts as an antifungal and antibacterial.

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively . GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, inclu

ML390 is a human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ML390 bioactivity: ER-HOX-GFP (EC50 μM) = 1.8 ± 0.6; U937 (EC50 μM) = 8.8 ± 0.8; THP-1 (EC50 μM) = 6.5 ± 0.9; DHODH (IC50, μM) = 0.56 ± 0.1. ML390 may offer insight into the mechanism of overcoming differentiation arrest, and will translate into a starting point for a much-needed new and potent treatment for patients with acute myeloid leukemia. Inhibitors of dihydroorotate dehydrogenase (DHODH) showed activity to induce differentiation in multiple animal models of AML in vitro and in vivo. DHODH inhibitors demonstrated effective at prolonging survival in animal models of leukemia.

GSK481 is a Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitor (RIP1 inhibitor). The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to

WEHI-539 is a highly potent and selective BCL-XL inhibitor. The prosurvival BCL-2 family protein BCL-X(L) is often overexpressed in solid tumors and renders malignant tumor cells resistant to anticancer therapeutics. WEHI-539 has high affinity (subnanomolar) and selectivity for BCL-X(L) and potently kills cells by selectively antagonizing its prosurvival activity. WEHI-539 will be an invaluable tool for distinguishing the roles of BCL-X(L) from those of its prosurvival relatives, both in normal cells and notably in malignant tumor cells, many of which may prove to rely upon BCL-X(L) for their sustained.

SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 Inhibitor, SIS3 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.

CITCO is a potent constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). CITCO altered expression of key drug-metabolizing enzymes and transporters in human hepatocytes, which positively affects the metabolic profile of CHOP. Coadministration of CITCO and CHOP in the coculture model led to significantly enhanced cytotoxicity in lymphoma cells but not in cardiomyocytes. Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss. The constitutive androstane receptor (CAR and NR1i3) is a key regulator of CYP2B6.

TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR. The most potent known member of the phenobarbital-like class of CYP-inducing agents. TCPOBOP has been used for enhancing Mcl-1-Italics promoter functions in mouse hepatoma cells. TCPOBOP has also been used to study constitutive androstane receptor(CAR)-induced gene expression in mouse hepatocytes.

GSK864 is a potent and selective inhibitor of mutant IDH1. GSK864 inhibits IDH1 mutants R132C/R132H/R132G with IC50 values of 9/15/17 nM, respectively, and is moderately selective over wild-type IDH1 and IDH2 mutants/wild-type. Treatment of R132C IDH1 mutant HT-1080 cells for 24 hours with GSK864 results in a dose-dependent reduction of 2-hydroxyglutarate (2-HG), which is not observed with GSK990, a structurally similar compound which is inactive as an IDH1 inhibitor. GSK864 has been shown to be selective in vitro for IDH1 over other classes of proteins (7TMs, ion channels, kinases) and chemoproteomic studies with GSK321, an analog of GSK864, confirm selective binding of IDH1 by this chemical series. GSK864 has a pharmacokinetic profile suitable for in vivo studies.

PD-161570 is a selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). PD 161570 had about 5- and 100-fold greater selectivity toward the FGF-1 receptor (IC50 = 40 nM) compared with the PDGFbeta receptor (IC50 = 262 nM) or EGF receptor (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture. The results demonstrate a novel synthetic inhibitor with nanomolar potency and specificity towards the FGF-1 receptor tyrosine kinase.

BTdCPU is an activator of HRI. The eIF2-alpha kinase HRI is a novel therapeutic target in multiple myeloma. Combination therapy with rapamycin, an mTOR inhibitor, and BTdCPU, an activator of HRI, demonstrated additive effects on apoptosis in dex-resistant cells. Thus, specific activation of the eIF2α kinase HRI is a novel therapeutic target in MM that can augment current treatment strategies.

UNC2541 is a potent and MerTK-specific inhibitor that exhibits sub-micromolar inhibitory activity in the cell-based ELISA. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket. UNC2541 showed IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM.

MYCi975, also known as NUCC-0200975, is a potent and selective MYC Inhibitor. MYCi975 disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression.

MYCi361, also known as NUCC-0196361, is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 suppresses tumor growth and enhances anti-PD1 immunotherapy.

CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate

DCN10809, also known as Paclitaxel succinate NHS ester, is a paclitaxel derivative with a succinic acid linker, in which the carboxy group is activated with an NHS ester. The NHS ester group is highly reactive to amino group or hydroxy group, and can be used to conjugate with other molecules such as peptides, proteins, antibodies or enzymes, or polymers. Paclitaxel-Succinic acid is a useful agent to make Paclitaxel-conjugate for drug delivery, nanodrug research.

CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 treatment resulted in significant growth inhibition, clonogenic survival, tumorsphere formation, and invasion of breast cancer cells. CADD522 negatively regulated transcription of RUNX2 target genes such as matrix metalloproteinase-13, vascular endothelial growth factor and glucose transporter-1, but upregulated RUNX2 expression by increasing RUNX2 stability. CADD522 reduced RUNX2-mediated increases in glucose uptake and decreased the level of CBF-β and RUNX2 phosphorylation at the S451 residue.

Didesmethylrocaglamide is a naturally occurring 1H-cyclopenta[b]benzofuran lignans of the rocaglamide type isolated from three Aglaia species (Aglaia duperreana, A. oligophylla and A. spectabilis). Didesmethylrocaglamide inhibited cell growth in a similar concentration range as the well-known anticancer drug vinblastine sulfate. Didesmethylrocaglamide arrested MPNST cells at G2-M, increased the sub-G1 population, induced cleavage of caspases and PARP, and elevated the levels of the DNA-damage response marker γH2A.X, while decreasing the expression of AKT and ERK1/2, consistent with translation inhibition.

Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

Trandolaprilat is a non-sulfhydryl angiotensin-converting enzyme inhibitor.

Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment.

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor. It can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

(-)-Cotinine is a major metabolite of nicotine in humans, it is a minor alkaloid found in tobacco plants.

LUF6283 is a partial agonist of hydroxycarboxylic acid receptor 2

CMS121 is a substituted quinoline that has neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities.

YE-120 is an agonist of G protein-coupled receptor 35 (GPR35).

TPT-172, also known as R33 (described in Mecozzi et al' s paper), is a thiophene thiourea derivative with molecule weight 172 in free base form. There is no formal name yet, we temporally call this molecule as TPT-172.

Idalopirdine, also known as Lu AE58054 or Iladopirdine, is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia. It is in phase III clinical trials. Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. Lu AE58054 demonstrated >50-fold selectivity for more than 70 targets examined. Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. Lu AE58054 may be useful for the pharmacotherapy of cognitive dysfunction in disease states such as schizophrenia and Alzheimer's disease.

BAM15 is a potent and selective mitochondrial uncoupler or protonophore. Chemical mitochondrial uncouplers are lipophilic weak acids that transport protons into the mitochondrial matrix via a pathway that is independent of ATP synthase, thereby uncoupling nutrient oxidation from ATP production. These uncouplers have potential for the treatment of diseases such as obesity, Parkinson’s disease, and aging.

CTP354, also known as C-21191, a novel deuterated subtype-selective GABA(A) modulator. CTP may be potentially useful for treatment of neuropathic pain, spasticity and anxiety disorders. GABAA receptors are found in the nervous system and, when activated, reduce the transmission of certain nerve signals. Several classes of widely used drugs target GABAA receptors, including benzodiazepines, but do not have the receptor subtype selectivity of CTP-354.

PF-06260414 is a selective androgen receptor modulator, or SARM, which is developed to treat muscle weakening. Testosterone’s anabolic properties help develop muscle mass, and its androgenic activity is associated with reproduction. Improving muscle mass would improve quality of life and may even prolong survival in certain patient populations.

DY-268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM). It does not display any FXR agonistic activity and cytotoxicity.

Cytosporone B is the first naturally occurring agonist for nuclear orphan receptor Nur77. The molecule binds with high affinity (IC50=0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities. Nur77 is also involved in glucose homeostasis, where it induces genes involved in gluconeogenesis. Csn-B physically binds to Nur77 and activates its transactivational activity and translocation to mitochondria to induce apoptosis. It inhibits cancer cell proliferation and tumor growth.

AM-2232 is a drug that acts as a potent but unselective agonist for the cannabinoid receptors.

AMG 009 is an orally active, small molecule CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) and DP (D prostanoid) dual antagonist, which was in preclinical development in the US for the treatment of asthma and allergic rhinitis.

Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.

SM16 is a novel Type I TGF-β signaling inhibitor.

Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.

NNC63-0532 is a potent and selective non-peptide agonist of the NOP receptors.

RL648_81 is a novel potent and selective activator of KCNQ2/3 channels.

TH1020 is a novel Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitor with promising activity (IC50 =0.85±0.12?μm) and specificity. TH1020 was shown to repress the expression of downstream TNF-α signaling pathways mediated by the TLR5/flagellin complex formation. Based on molecular docking simulation, TH1020 is suggested to compete with flagellin and disrupt its association with TLR5. TH1020 provides a much-needed molecular probe for studying this important protein-protein interaction and a lead compound for identifying novel therapeutics targeting TLR5.

5-BDBD is a selective inhibitor of P2X4.

CPT is a potent adenosine A1 receptor antagonist.

PHA-543613 acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.

Glibornuride is a blocker of adenosine 5'-triphosphate (ATP)-sensitive K+ channels (KATP channels).

A-350619 hydrochloride is an activator of soluble guanylyl cyclase (sGC).

SCH-23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). SCH-23390 is also an agonist at 5-HT1C and 5-HT2C receptors in vitro (Ki values are 6.3 nM and 9.3 nM respectively). It blocks quinpirole-induced Kir3 (GIRK) currents (EC50 = 268 nM) independently of receptors.

GNE-140 racemic is a novel potent lactate dehydrogenase (LDHA) inhibitor. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance.

CP-24879 hydrochloride is a D5D/D6D dual-inhibitor, showing beneficial effects against increased intracellular lipid accumulation and inflammatory injury in hepatocytes.

CRANAD-2 is a difluoroboron-derivatized curcumins as near-infrared probe for in vivo detection of amyloid-beta deposits. Upon interacting with Abeta aggregates, CRANAD-2 undergoes a range of changes, which include a 70-fold fluorescence intensity increase, a 90 nm blue shift (from 805 to 715 nm), and a large increase in quantum yield. Moreover, this probe also shows a high affinity for Abeta aggregates (K(d) = 38.0 nM), a reasonable log P value (log P = 3), considerable stability in serum, and a weak interaction with albumin. After intravenous injection of this probe, 19-month-old Tg2576 mice exhibited significantly higher relative signal than that of the control mice over the same period of time.

MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications.

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition. The observed parallel rightward shift of concentration-response curves with different antagonist concentrations is consistent with a competitive binding mode. Since R0 46-8443 selectively inhibits ETB receptor mediated responses, it is a valuable tool for clarifying the role of ETB receptors in pathology.

(-)-Isoproterenol hydrochloride is an agonist of beta-adrenergic receptor. (-)-Isoproterenol hydrochloride is also used in the treatment of bradycardia; bronchodilator.

NCDM-32B is a novel potent and selective KDM4 inhibitor, impairing viability and transforming phenotypes of basal breast cancer.

Naltriben is a highly selective δ2 opioid receptor antagonist.Naltriben (NTB) has been used to differentiate the subtypes of delta opioid receptors, delta1 and delta2. NTB displaced the specific binding of [3H]DAMGO with Ki value of 19.79 +/- 1.12 nM in rat cortex membranes. Specific binding of [3H]diprenorphine ([3H]DIP) was inhibited by NTB with Ki value of 82.75 +/- 6.32 nM in the presence of DAMGO and DPDPE. Naltriben enhanced the MAPK/ERK signaling pathway, but not the PI3k/Akt pathway. Therefore, potentiated TRPM7 activity contributes to the devastating migratory and invasive characteristics of GBM.

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist potentially for the treatment of solid tumors.

ONO-8130 is an orally available EP1 receptor antagonist.

Adaphostin is a novel activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia.

Espindolol is a β-adrenoceptor antagonist potentially for the treatment of cachexia related to cancer.

Alpha-Lipoic Acid Choline Ester, also known as alpha-LACE, EV-06 or UNR844, is a drug candidate potentially for the treatment of presbyopia. Alpha-LACE was designed to permeate biological membranes with the incorporation of the cationic choline head grou

GW-870086 is a glucocorticoid receptor agonist potentially for the treatment of asthma and atopic dermatitis.

C16, also known as GW-506033X or PKR Inhibitor. C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. GW-506033X protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress. PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. PKR inhibitor C16 binds efficiently with human microtubule affinity-regulating kinase 4.

JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.

MitoPQ, also known as MitoParaquat, is a redox cycler. MitoParaquat (MitoPQ) that comprises a triphenylphosphonium lipophilic cation conjugated to the redox cycler paraquat. MitoPQ accumulates selectively in the mitochondrial matrix driven by the membrane potential. Within the matrix, MitoPQ produces superoxide by redox cycling at the flavin site of complex I, selectively increasing superoxide production within mitochondria. MitoPQ increased mitochondrial superoxide in isolated mitochondria and cells in culture ~a thousand-fold more effectively than untargeted paraquat. MitoPQ was also more toxic than paraquat in the isolated perfused heart and in Drosophila in vivo. MitoPQ enables the selective generation of superoxide within mitochondria and is a useful tool to investigate the many roles of mitochondrial superoxide in pathology and redox signaling in cells and in vivo.

PF-06279794, also known as PF-794, is a potent, selective and ATP-competitive TNIK inhibitor.

H-89 is a specific adenylyl cyclase inhibitor (DDA) and a cyclic AMP-dependent protein kinase inhibitor. H-89 blocks the action of equine growth hormone on in vitro maturation of equine oocytes. H-89 decreases the gain of excitation-contraction coupling and attenuates calcium sparks in the absence of beta-adrenergic stimulation. H-89 potentiates adipogenesis in 3T3-L1 cells by activating insulin signaling independently of protein kinase A.

JIB-04 Z-isomer, also known as NSC 693627, is an isomer of JIB-04. JIB-04 is a Jumonji histone demethylase inhibitor. JIB-04 selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. JIB-04 can prolong survival in a mouse model of breast cancer.

TCN-201 is a selective antagonist of NMDA receptors containing the NR2A subunit. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.

GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively).

nor-NOHA is a potent, selective, competitive, and high affinity inhibitor of arginase. nor-NOHA inhibits arginase from rat liver (IC50 = 2 μM) and mouse macrophages (IC50 = 50 μM).

N-Formyl-Met-Leu-Phe, also known as fMLF, is a potent neutrophil chemoattractant and the reference agonist for the G protein-coupled N-formylpeptide receptor (FPR).

Benzethonium Chloride, also known as Hyamine, is synthetic quaternary ammonium salt that has surfactant, antiseptic, and anti-infective properties. Benzethonium Chloride is commonly used as a topical antimicrobial agent. Benzethonium chloride exhibited concentration-dependent inhibitions of HERG channel currents with IC(50) values of 4nM and 17nM, respectively, which were also voltage-dependent and use-dependent. Benzethonium Chloride shifted the channel activation I-V curves in a hyperpolarized direction for 10-15mV and accelerated channel activation and inactivation processes by 2-fold.

PF9601N is a selective and potent monoamine oxidase B inhibitor that exhibit anti-Parkinsonian effects in several models of PD.

A286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

PE 154 are known to associate with β-amyloid plaques, and histological co-localization of AChE and Ab peptides is well established in Alzheimer’s disease. PE-154 is a fluorescent inhibitor of both AChE and BChE with IC50 values of 280 pM and 16 nM. PE-154 stains Aβ plaques in both rodent and human tissue samples, and does not cross react with phospho-tau.

AZ12216052 is a mGluR II and III activator.

BIBF-1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.

FK-888 is a selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. FK-888 inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo.

L-765,314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.

LSN2463359 is a novel positive allosteric modulators of the mGlu? receptor.

MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.

MRS1220 is a potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. MRS1220 displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors.

PSB1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. It produces potent analgesic effects in vivo.

PSB603 is a adenosine A(2B) receptor antagonist which suppresses tumor growth and metastasis by inhibiting induction of regulatory T cells.

Amphotericin B binds ergosterol and induces membrane pore formations, increasing ROS and suppressing fungal growth. It also increases expression of IL-1-beta, TNF-alpha, BDNF and GDNF and protects against prion-induced neurodegeneration.

Arvanil is a CB1 and TRPV1 agonist. It increases lung tidal volume, diaphragm activity, mean arterial blood pressure and inhibits lymphocyte proliferation.

O(6)-Benzylguanine is an MGMT inhibitor that prevents the repair of DNA damage induced by chemotherapeutics. It allows apoptosis and other mechanisms of cell death to occur.

Erucin is a sulforaphane analog and telomerase inhibitor found in cruciferous vegtables. It induces phase II enzyme activity, suppresses cellular proliferation in hepatocellular carcinoma cells, prevents 6-OHDA-induced neurodegenration, and inhibits LPS-s

Calcium saccharate is an oxidized non-cyclic hexose sugar. It may inhibit carcinogenesis and proliferation of cancer cells.

GSK 2830371 is a WiP1 inhibitor. It inhibits cell growth and tumor growth in lymphoma and neuroblastoma models.

D-Luciferin sodium is heterocyclic light-emitting compound and natural ligand for luciferase used to detect cell activity. It requires ATP for its reaction, emitting a greenish-yellow luminescence at a peak wavelength of approximately 530 nm. The salt form of luciferin dissolves in water or other typical buffers.

Marbofloxacin is a bacterial DNA gyrase inhibitor. It suppresses growth of Staphylococus, Escherichia, Actinobacillus, Pasturella, and Mannhemia.

NMS-E973 is a novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). NMS-E973 displays significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile. The efficacy profile of NMS-E973 suggests a potential for development in different clinical settings, including tumors that have become resistant to molecular targeted agents, particularly in cases of tumors which reside beyond the blood-brain barrier (BBB).

Chlorfenson is used to treat onychomycosis (nail fungus) as the primary indication.

SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice.

Anavex2-73 is a muscarinic/σ1 ligand. ANAVEX2-73 (0.01-3.0 mg/kg i.p.) alleviated the scopolamine- and dizocilpine-induced learning impairments. ANAVEX2-73 (300 μg/kg) also reversed the learning deficits in mice injected with Aβ(25-35) peptide, a non-transgenic Alzheimer's disease model. The neuroprotective activity of ANAVEX2-73, its mixed cholinergic/σ(1) activity, its low active dose range and its long duration of action together reinforce its therapeutic potential in Alzheimer's disease.

L-p-Bromotetramisole is a cell-permeable inhibitor of all four human AP isoenzymes (Kis =18 and 56 μM for PLAP and NSAP, respectively).

CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

LJ570 is the first PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. LJ570 is a potent partial agonist of both PPARα and γ subtypes. LJ570 inhibited the Cdk5-mediated phosphorylation of PPARγ at serine 273 that is currently considered the mechanism by which some PPARγ partial agonists exert antidiabetic effects similar to thiazolidinediones, without showing their typical side effects. LJ570 may be useful for treatment of dyslipidemic type 2 diabetes.

RO2959 is a novel, potent and selective CRAC current inhibitor. RO2959 completely inhibited cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction). RO2959 potently blocked TCR triggered gene expression and T cell functional pathways similar to CsA and another calcineurin inhibitor FK506.

DODMA, also known as MBN 305A is a a cationic lipid containing the unsaturated long-chain (18:1) oleic acid inserted at both the sn-1 and sn-2 positions. It has been used in the composition of lipospomes formulated as stable nucleic acid lipid particles that can encapsulate siRNA or other small molecules to be used for drug delivery