| DC75455 |
XE991 free base |
XE991, also known as LS190926, is a potent and selective KCNQ channel blocker. XE991 blocks KCNQ2+3/M-currents (IC50 = 0.6-0.98 μM) and KCNQ1 homomeric channels (IC50 = 0.75 μM) but is less potent against KCNQ1/minK channels (IC50 = 11.1 μM). |
|
| DC75456 |
Aminolevulinic Acid HCl |
Aminolevulinic acid, also known as ALA, is a topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid (ALA) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect. In 1999, FDA approved this drug for for actinic keratosis. |
|
| DC75457 |
Abiraterone Acetate |
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. |
|
| DC75458 |
Ulixertinib (BVD-523) |
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. |
|
| DC75459 |
INCB14943 |
INCB14943, also known as INCB024360-analog, IDO5L and IDO-IN-2 with CAS#914471-09-3, is a potent and orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1) with potential immunomodulating and antineoplastic activities. INCB024360-analog is a potent (HeLa IC50=19 nM) competitive inhibitor of IDO. Testing of INCB024360-analog in mice demonstrated pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy. ||Note: MedKoo CAT#206461, INCB024360 has CAS#1204669-58-8 (http://www.medkoo.com/products/6778) |
|
| DC75460 |
Palbociclib HCl |
Palbociclib, also known as PD0332991, is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases. It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest at nanomolar concentrations. |
|
| DC75461 |
Crizotinib |
Crizotinib, also known as PF-02341066, is an orally bioavailable agent belonging to the class of c-met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors with potential antineoplastic activity. Crizotinib was approved for treatment of some non-small cell lung carcinoma (NSCLC) in the US, and undergoing clinical trials testing its safety and efficacy in anaplastic large cell lymphoma, neuroblastoma, and other advanced solid tumors in both adults and childre. Crizotinib inhibits the membrane receptor MET and activation of the MET signaling pathway, which may block tumor cell growth, migration and invasion, and tumor angiogenesis in susceptible tumor cell populations. Crizotinib was approved in 2011. |
|
| DC75462 |
Lerociclib |
Lerociclib , also known as G1T38, is an oral, potent and selective CDK4/6 inhibitor for the treatment of Rb competent tumors. Biochemical profiling demonstrates G1T38 is a competitive, nanomolar inhibitor of CDK4/6 with highly selectivity for CDK4-cyclin D1 and CDK6-cyclin D3. G1T38 exhibits a low EC50 (<100 nM) in Rb competent cell lines compared to >3 μM in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models. |
|
| DC75463 |
K-7174-2HCl |
K-7174 is a novel orally active, potent proteasome inhibitor. K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib. K-7174 is also a GATA-specific inhibitor, which may have potential application in treating anemia of chronic disease. |
|
| DC75464 |
Enarodustat |
Enarodustat, also known as JTZ-951, is a prolyl hydroxylase inhibitor. JTZ-951 (enarodustat) stabilizes HIF-α protein and induces erythropoiesis without effects on the function of vascular endothelial growth factor. Enarodustat increases endogenous erythropoietin levels in the treatment of anemia associated with chronic kidney disease (CKD). JTZ-951 induces erythropoiesis without affecting VEGF function. JTZ-951 may be a new oral candidate that increases and maintains hemoglobin concentrations in renal anemia patients. |
|
| DC75465 |
Rupitasertib free base |
Rupitasertib, also known as M2698, MSC-2363318A, is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier. M2698 was highly potent in vitro (IC50 1 nM for p70S6K, Akt1 and Akt3 inhibition; IC50 17 nM for pGSK3β indirect inhibition) and in vivo (IC50 15 nM for pS6 indirect inhibition), and relatively selective (only 6/264 kinases had an IC50 within 10-fold of p70S6K). |
|
| DC75466 |
Elsulfavirine free base |
Elsulfavirine is a new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) being developed by Viriom for the treatment and prevention of human immunodeficiency virus (HIV) infections. It is the prodrug of the active compound VM-1500A, a small molecule selective NNRTI, which prevents HIV replication. In June 2017, elsulfavirine received its first global approval in Russia for the treatment of HIV-1 infections in combination with other antiretroviral medicines. Other formulations of this drug are also being evaluated in preclinical and phase II studies for the treatment of HIV infections and/or pre-exposure and post-exposure prophylaxis. |
|
| DC75467 |
Aldoxorubicin HCl |
Aldoxorubicin, also known as INNO-206 and Doxo-EMCH, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin with antineoplastic activity. INNO-206 binds selectively to the cysteine-34 position of albumin via its maleimide moiety. Doxorubicin is released from the albumin carrier after cleavage of the acid-sensitive hydrazone linker within the acidic environment of tumors and, once located intracellularly, intercalates DNA, inhibits DNA synthesis, and induces apoptosis. Albumin tends to accumulate in solid tumors as a result of high metabolic turnover, rapid angiogenesis, hyervasculature, and impaired lymphatic drainage. Because of passive accumulation within tumors, this agent may improve the therapeutic effects of doxorubicin while minimizing systemic toxicity. NOTE: Current batch has ~90% purity by HPLC. The rest 10% is doxouribin HCl. |
|
| DC75468 |
GW438014 free base |
GW438014A is a selective NPY-Y5 receptor antagonist. |
|
| DC75469 |
Irinotecan Free base |
Irinotecan Free base is a camptothecin analog and topoisomerase I inhibitor. It may inhibit AChE. It is uesed to treat colon cancer, but it also moderates inhibition of dendritic cell differentiation and decreases the number of tumor vessels in glioma models. |
|
| DC75470 |
Desvenlafaxine Succinate hydrate |
Desvenlafaxine Succinate is a venlafaxine metabolite and inhibitor of SERT and NET used to treat depression. It also alters rates of gastric emptying and decreases symptoms of menopausal hot flashes. |
|
| DC75471 |
Norepinephrine bitartrate hydrate |
Norepinephrine is an organic chemical in the catecholamine family that functions in the human brain and body as a hormone and neurotransmitter. Norepinephrine directly stimulates adrenergic receptors. Stimulation of alpha-adrenergic receptors causes vasoconstriction of the radial smooth muscle of the iris, arteries, arterioles, veins, urinary bladder, and the sphincter of the gastrointestinal tract. Stimulation of beta-1 adrenergic receptors causes an increase in myocardial contractility, heart rate, automaticity, and atrioventricular (AV) conduction while stimulation of beta-2 adrenergic receptors causes bronchiolar and vascular smooth muscle dilatation. |
|
| DC75472 |
Indinavir sulfate |
Indinavir sulfate is an inhibitor of HIV protease, GLUT4, and calpain used to treat HIV infection. It also decreases phosphorylation of the insulin receptor β subunit, inhibits adenocarcinoma tumor growth, and may induce SOCS1 signaling. |
|
| DC75473 |
R-IMPP |
R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. |
|
| DC75474 |
Necrosulfonamide |
Necrosulfonamide is a novel inhibitor of MLKL (mixed lineage kinase domain-like). Necrosulfonamide is a cell-permeable inhibitor that covalently modifies Cys88 and blocks human MLKL adaptor function. Necrosulfonamide Attenuates Spinal Cord Injury via Necroptosis Inhibition. |
|
| DC75475 |
Saccharin 1-methylimidazole |
Saccharin 1-methylimidazole, also known as SMI, is a chemical activator commonly used in solid-phase synthesis of DNA and RNA oligonucleotides. Saccharin 1-methylimidazole has been used to synthesize single-stranded DNA oligonucleotides that are resistant to nuclease digestion. |
|
| DC75476 |
Batimastat |
Batimastat (also known as BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Matrix metalloproteinases (MMPs) are thought to play a significant role in tumor invasion and metastasis as well as angiogenesis. Batimastat, also known as BB-94, acts as an inhibitor of metalloproteinase activity by binding the zinc ion in the active site of MMPs. |
|
| DC75477 |
Nintedanib |
Nintedanib, also known as BIBF 1120, is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR). Intedanib selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. On 11/15/2014 , FDA approved Nintedanib for the treatment of idiopathic pulmonary fibrosis (IPF). |
|
| DC75478 |
Alectinib free base |
Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Alectinib was approved in Dec. 2015. |
|
| DC75479 |
Daunorubicin hydrochloride |
Daunorubicin hydrochloride is the hydrochloride salt of an anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. |
|
| DC75480 |
Amodiaquin HCl hydrate |
Amodiaquin dihydrochloride is an inhibitor of the Ebola virus. It acts by targeting the viral protein 35 (VP35). |
|
| DC75481 |
Vidofludimus |
Vidofludimus, also known as 4SC 101 or SC12267, is a novel orally active and potent DHODH inhibitor. In vitro, 4SC-101 is a potent inhibitor of human DHODH, inhibits lymphocyte proliferation, and uniquely blocks phytohemagglutinin-stimulated IL-17 production by lymphocytes. In vivo, oral administration of 4SC-101 effectively improved both chronic DSS and acute TNBS colitis in mice. 4SC-101 may have potential for the treatment of intestinal inflammation. Dihydroorotate dehydrogenase (DHODH) is a key enzyme involved in pyrimidine biosynthesis. DHODH is a known target for the treatment of autoimmune diseases. |
|
| DC75482 |
LYS01 free base |
LYS01 free base is a new lysosomal autophagy inhibitor. Lys01 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. The trihydydrochloride salt of LYS01 is called LYS05. Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome, resulting in impaired autophagy and tumor growth. |
|
| DC75483 |
S14506 HCl |
S 14506 is a highly potent selective 5-HT1A receptor full agonist (pKi values are 9.0, 6.6, 7.5, 6.6 and < 6.0 for 5-HT1A, 5-HT1B, 5-HT1C, 5-HT2 and 5-HT3 receptors respectively). It potentially binds between the agonist binding site and the G protein interaction switch site, affecting the activation mechanism, and may display positive cooperativity. |
|
| DC75484 |
Desmethyl-VS-5584 |
Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. |
|
