L 709049 is a biochemical.

Josamycin is a macrolide antibiotic.

Midecamycin is a naturally occurring 16-membered macrolide that fits under the category of acetoxy-substituted macrolide antibiotics. In this molecule, an acetoxy group is substituted on the position 9 of the 16-member ring and on position 4 of the terminal sugar.

Oxazole yellow is a fluorescent cyanine dye that binds to DNA and is used to detect apoptotic cells. Oxazole yellow does not enter live cells. However, during apoptosis the cytoplasmic membrane becomes slightly permeable, allowing entry of the dye. Oxazole yellow is often used along with propidium iodide (catalog no. P4170), a DNA dead cell stain that does not enter either live or apoptotic cells. The λEx/λEm of Oxazole yellow is 491/509.

Alizarine Yellow R is a yellow colored azo dye made by the diazo coupling reaction.

Calcon is a biochemical indicator of calcium.

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.

DMH4 is a potent VEGF inhibitor and an angiogenesis inhbitor.

GW2974 Potent and selective dual inhibitor of EGFR.

NP603 is a cell-permeable inhibitor of PDGFRβ, FGFR1 and VEGFR2 that binds to ATP pocket. NP603 is a very weak inhibitor of EGFR

PD173952 is a Src family kinase inhibitor.

PF-06250112 is a potent inhibitor of Bruton′s tyrosine kinase

PF-06439015 is a potent and selective inihibitor that overcomes clinical ALK (receptor tyrosine kinase anaplastic lymphoma kinase) mutations resistant to Crizotinib.

Roslin 2 is a p53 reactivator that disrupts the FAK and p53 interaction, and reactivates transcriptional activity of p53 with p21, Mdm-2 and Bax transcriptional targets. Roslin 2 decreases viability and clonogenicity of cancer cells, and inhibits tumor growth.

SKI 5C is a selective Sphingosine Kinase 1 (SPHK1) inhibitor.

Tyrphostin 51 is a potent inhibitor of EGFR (EGF receptor) kinase activity

Tyrphostin AG 1112 is a Bcr-Abl kinase blocker that can activate the terminal differentiation of K562 cells and the purging of Ph+ cells.

Tyrphostin AG 825 is shown to be a potent inhibitor of EGFR (epidermal growth factor receptor) and Neu (HER-2) kinases.

Rescinnamine is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug. It is a vinca alkaloid obtained from Rauwolfia serpentina and other species of Rauwolfia.

Tazobactam sodium is a biochemical.

Methylmethionine sulfonium chloride is a biochemical.

Methoprene is a juvenile hormone (JH) analog which acts as a growth regulator when used as an insecticide. It is an amber-colored liquid with a faint fruity odor which is essentially nontoxic to humans when ingested or inhaled. It is used in drinking water cisterns to control mosquitoes which spread dengue fever and malaria.

Aurodox is a polyketide antibiotic active against Gram-positive bacteria. It is effective against S. pyogenes infection in mice with a 50% curative dose (CD50) value of 71 mg/kg. Aurodox inhibits bacterial protein synthesis by binding to bacterial elongation factor Tu (EF-Tu) and inhibiting its release from the ribosome.

Ranitidine-S-oxide is a metabolite of Ranitidine. Ranitidine, sold under the trade name Zantac among others, is a medication which decreases stomach acid production. It is commonly used in treatment of peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome.

Xanthinol niacinate is a combination of xanthinol and niacin which acts as a vasodilator. Studies show that Xanthinol niacinate can modulate tumors during their reoxygenation. Xanthinol niacinate also displays anti-platelet and thrombolytic activity. In addition, this compound can reduce whole blood viscosity, as a result of its anti-platelet activity and decrease cholesterol and fibrinogen.

Dixanthogen is an ectoparasiticide.

Xantphos is an organophosphorus compound derived from the heterocycle xanthene.

Rhodamine 110 is a biochemical.

Rhodamine 123 is a chemical compound and a dye.

Fenazaquin is a chemical compound from the group of quinazoline derivatives and alkylaryl ethers

Cyhalofop-butyl is a biochemical.

Tetrasulis a chemical compound from the group of thioethers and diphenyls .

Flutianil is a chemical compound from the group of thiazolidines .

Penicillin V potassium is a broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.

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

Bromopride is a dopamine antagonist with prokinetic properties widely used as an antiemetic

Prenylamine is a calcium channel blocker of the amphetamine chemical class which was used as a vasodilator in the treatment of angina pectoris.

Valencene is a sesquiterpene that is an aroma component of citrus fruit and citrus-derived odorants.

Isocaproaldehyde is a biochemical.

Vamidothion sulfoxide is a biochemical.

Mexacarbate is a carbamate pesticide developed by Alexander Shulgin.

Chlorpyrifos-methyl acts on the nervous system of insects by inhibiting acetylcholinesterase.

MCPA-thioethyl is a biochemical.

Vapiprost hydrochloride is a biochemicla.

Clopyralid is a selective herbicide used for control of broadleaf weeds.

Clothiapine, also known as Entumine, is an atypical antipsychotic of the dibenzothiazepine chemical class. It was first introduced in a few European countries (namely, Belgium, Italy, Spain and Switzerland), Argentina, Taiwan and Israel in 1970.

Crimidine is a convulsant poison used as a rodenticide. Crimidine was originally known by its product name, Castrix. It was originally produced in the 1940s by the conglomerate, IG Farben.

Alclofenac may be used to treat patients with chronic rheumatic diseases. Research shows that alclofenac has a pronounced effect upon the acute-phase protein response and the extent to which L-tryptophan is bound to plasma protein.

Butachlor is a chloroacetanalide herbicide. Butachlor is commonly used for weed control in rice as well as cotton, maize, wheat and other crops.

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.

Vedaprofen is a nonsteroidal anti-inflammatory drug (NSAID) used in veterinary medicine for the treatment of pain and inflammation due to musculoskeletal disorders in dogs and horses and for the treatment of pain due to horse colic

Mefluidide is a biochemical.

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

FIIN-1 is Potent, irreversible FGFR inhibitor, acts at the ATP binding site. Also irreversibly inhibits Flt-1, Flt-4 and VEGFR-2.

OM137 is an inhibitor of Aurora kinases. which is growth inhibitory to cultured cells when applied at high concentration and potentiates the growth inhibitory effects of subnanomolar concentrations of paclitaxel.

YC-137 is a BCL-2 inhibitor, which selectively induces apoptosis of Bcl-2-overexpressing cells and disrupts its interaction with Bid BH3, thereby blocking the anti-apoptotic activity of Bcl-2.

PD166326 is one of the most potent members of the pyridopyrimidine class of protein tyrosine kinase inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl kinase activity after a single oral dose and demonstrated marked antileukemic activity in vivo. In vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.

PD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.

GTP-14564 is a specific kinase inhibitor for ITD-FLT3. GTP-14564 inhibited the growth of interleukin-3-independent Ba/F3 expressing ITD-FLT3 at 1 microM, whereas a 30-fold higher concentration of GTP-14564 was required to inhibit FLT3 ligand-dependent growth of Ba/F3 expressing wild type FLT3 (wt-FLT3).

KU59403 is a potent and selective ATM (Ataxia telangiectasia mutated) inhibitor with with potential anticancer activity. KU59403 was not cytotoxic to human cancer cell lines (SW620, LoVo, HCT116, and MDA-MB-231) per se but significantly increased the cytotoxicity of topoisomerase I and II poisons: camptothecin, etoposide, and doxorubicin. KU59403 significantly enhanced the antitumor activity of topoisomerase poisons in mice bearing human colon cancer xenografts (SW620 and HCT116) at doses that were nontoxic alone and well-tolerated in combination

CAY10505 is a phosphatidylinositol 3-kinase-γ inhibitor , was found to significantly improve acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. CAY10505 , may improve hypertension-associated vascular endothelial dysfunction. Inhibition of PI3Kγ might be a useful approach in the therapeutics of vascular endothelium dysfunction.

PD0407824, also known as PD407824 is a potent selective, small molecular CHK1 inhibitor with potential anticancer activity.

NU6140 is a cyclin-dependent kinase 2 (cdk2) inhibitor; induces cell-cycle arrest at the G2-M phase.

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

Methylthioadenosine, also known as MTA and 5'- Methylthioadenosine, is a naturally occurring sulfur-containing nucleoside present in all mammalian tissues. In vitro experiments showed that MTA treatment inhibited melanoma cell proliferation and viability in a dose dependent manner, where BRAF mutant melanoma cell lines appear to be more sensitive. Importantly, MTA was effective inhibiting in vivo tumor growth. The molecular analysis of tumor samples and in vitro experiments indicated that MTA induces cytostatic rather than pro-apoptotic effects inhibiting the phosphorylation of Akt and S6 ribosomal protein and inducing the down-regulation of cyclin D1. ( BMC Cancer . 2010 Jun 8;10:265.)

Purpurogallin is a red, crystalline compound, and the aglycon of several glycosides from nutgalls and oak barks. It can inhibit hydroxyestradiol methylation by catechol-O-methyltransferase. It potently and specifically inhibits PLK, TLR1/TLR2 activation pathway. Purpurogallin showed antiplatelet and antithrombotic activities; anti?inflammatory effects; antitumor activity, anti-oxidation activities; hepatoprotecting effects; antibacterial activity toward gram-positive bacteria.

Thiocolchicine is a potent tubulin polymerization and microtubule assembly inhibitor, a axonal cytoskeleton modulator and apoptosis inducer. Structurally, thiocolchicine is a colchicine analog in which the C-10 methoxy is replaced with a thiomethyl moiety. Thiocolchicine was shown to bind with high affinity to the colchicine site on tubulin (Ka = 1.07 +/- 0.14 x 10(6) M-1). Thiocolchicine-dimers were shown to be potent topoisomerase I inhibitors.

ATN-163 is a five amino acid peptide. ATN-163 is a scramble peptide of ATN-161. ATN-161 (Ac-PHSCN-NH2), a five-amino acid peptide with documented anti-angiogenic activity.

Gemcitabine monophosphate disodium salt, also called GemMP, is a monophosphate derivative of Gemcitabine. Gemcitabine (Gem) is a deoxycytidine analog that is effective against pancreatic cancer and other malignancies following conversion to the 5'-O-mono-, di- and tri-phosphate forms. GemMP decreased tumor cell growth at concentrations ranging from 1 to 50 nM. GemMP is a potent cytotoxic agent that serves to induce apoptosis in association with increased Fas expression in cultured thyroid cancer cell lines. (Anticancer Res. 2000 Sep-Oct;20(5A):2915-22).

9-hydroxyellipticine, also known as IGIG 929 and LS133324, is a potent cytotoxic and antitumor agent. Structurally, 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine. The hydroxy group in 9-hydroxyellipticines increases the apparent affinity for DNA, stabilisation of toposiomerase II-DNA cleavable complex, oxidation to reactive quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines.

Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. As a result, pyridostatin modulated the expression of these genes, including the proto-oncogene SRC.

Doxorubicin-SMCC, also known as ADR-SMCC, dox-SMCC, is a derivative of doxorubicin with a SMCC linker (Succinimidyl-4-( N -maleimidomethyl)cyclohexane-1-carboxylate). Maleimide in doxrubicin-SMCC can react with sulfhydryl groups at pH 6.5-7.5 to form a stable thioether bond. Doxorubicin-SMCC can be used to synthesize doxorubicin bioconjugates with proteins, enzymes; antobodies, antigens, and other biopolymers. Doxorubicin-SMCC is often used for drug delivery research.

MC1742 is a novel and selective HDAC inhibitor with potential anticancer activity. Musculoskeletal sarcomas are aggressive malignancies of bone and soft tissues often affecting children and adolescents. Histone deacetylase inhibitors (HDACi) have been proposed to counteract cancer stem cells (CSCs) in solid neoplasms. When tested in human osteosarcoma, rhabdomyosarcoma, and Ewing's sarcoma stem cells, the new HDACi MC1742 increased acetyl-H3 and acetyl-tubulin levels and inhibited CSC growth by apoptosis induction. At nontoxic doses, 1 promoted osteogenic differentiation. (copied from J Med Chem. 2015 Apr 30. [Epub ahead of print].

Nigericin is an antibiotic derived from Streptomyces hygroscopicus. Its isolation was described in the 1950s, and in 1968 the structure could be elucidated by X-ray crystallography. The structure and properties of nigericin are similar to the antibiotic monensin. Commercially it is obtained as a byproduct, or contaminant, at the fermentation of Geldanamycin. It is also called Polyetherin A, Azalomycin M, Helixin C, Antibiotic K178, Antibiotic X-464. Nigericin acts as an H+, K+, Pb2+ ionophore. Most commonly it is an antiporter of H+ and K+. In the past nigericin was used as an antibiotic active against gram positive bacteria. It inhibits the Golgi functions in Eukaryotic cells. Nigericin exhibits anticancer and anti-HIV activity.

Temozolomide Acid, also known as TMZA, is a metabolite of temozolomide (TMZ) with demonstrable anticancer activity in vitro. Temozolomide, (TMZ) (brand names Temodar and Temodal and Temcad) is an oral chemotherapy drug. It is an alkylating agent used as a treatment of some brain cancers; as a second-line treatment for astrocytoma and a first-line treatment for glioblastoma multiforme.

MC-70 is a potent P-gp inhibitor (EC50 = 0.69 μM). Multidrug resistance (MDR) is the major cause of the failure of cancer therapy since this phenomenon generates cancer cells that are unresponsive to chemotherapeutic agents. P-glycoprotein (P-gp) is a well-known membrane transporter expressed in a number of strategic biological barriers, where it exerts a protective effect of paramount importance.

Aluminum phthalocyanine disulfonate sodium, also known as AlPcS2 disodium or AlS2Pc or AlPcS(2a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum phthalocyanine disulfonate is a mixture of regional isomers, in which sulfonate group can be in 3- or 4- position in phenyl ring. Aluminum phthalocyanine disulfonate is also a Coloring Agent; Dermatologic Agent; Fluorescent Dye; Indicators and Reagent; Luminescent Agent; Photosensitizing Agent; Radiation-Sensitizing Agent.

AlPcS4 , also known as aluminum phthalocyanine tetrasulfonate Chloroaluminum tetrasulfophthalocyanine; or AlS4Pc, AlPcS4(a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum phthalocyanine disulfonate is a mixture of regional isomers, in which sulfonate group can be in 3- or 4- position in phenyl ring. Aluminum phthalocyanine disulfonate is also a Coloring Agent; Dermatologic Agent; Fluorescent Dye; Indicators and Reagent; Luminescent Agent; Photosensitizing Agent; Radiation-Sensitizing Agent.

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

Bromopyruvic acid is a hexokinase II inhibitor and an effective antitumor agent. The characteristics of 3-bromopyruvate in vitro and in vivo have been reported in the scientific literature since the 1940s. Because it is a highly reactive alkylating agent and it is inherently unstable, it had been described as a metabolic poison. Research at Johns Hopkins has suggested that 3-bromopyruvate could be used to selectively kill cancer cells, while leaving normal cells intact. Recently, the FDA accepted an IND application for the use of 3-bromopyruvate for a Phase I clinical trial in liver cancer. IMPORTANT NOTE: this product we are offering is a pure chemical solid powder, which is for research use only, not for human or therapeutic use. Buyer must be a professional and understands how to use and handle the chemical properly.

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.

GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1). GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns. GSK-LSD1 inhibits LSD1 with an IC50 of 16 nM and is > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). GSK-LSD1 induces gene expression changes in cancer cell lines (average EC50 < 5 nM) and inhibits cancer cell line growth (average EC50 < 5 nM). Lysine specific demethylase 1 (LSD1) is a histone demethylase found in various transcriptional co-repressor complexes. LSD1 is involved in ES cell differentiation, hematopoiesis, and has been described as having a role in Acute Myeloid Leukemia (AML). (http://www.thesgc.org/chemical-probes/GSK-LSD1)

Aloisine A is a potent and selective CDK/GSK-3 inhibitor. Aloisine A inhibits cell proliferation by arresting cells in both G1 and G2. IC50 data of Aloisine A: Cdc2 (CDK1)/cyclin B (IC50 = 150nM), Cdk2/cyclin A (IC50 = 120nM), Cdk2/cyclin E (IC50 = 400nM), Cdk5/p25 (IC50 = 200nM), Cdk5/p35 (IC50 = 160nM), and GSK-3α (IC50 = 500nM). Aloisine A also inhibits GSK-3β (IC50 = 650nM) and JNK (c-Jun N-terminal kinase) (IC50~3-10μM). Aloisine A blocks the cell cycle in both G1 and G2 phase.

MTDIA, also known as MT-DADMe-ImmA, and Methylthio-DADMe-Immucillin A, is a MTAP inhibitor. Human 5'-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5'-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage. Transition-state (TS) analogues of MTAP are in development as anticancer candidates. TS analogues of MTAP incorporate a cationic nitrogen and a protonated 9-deazaadenine leaving group, which are mimics of the ribocation transition state. MT-ImmA and MT-DADMe-ImmA are two examples of these TS analogues.

5'-deoxyadenosine, also known as 5'dAdo or 5'-dAdo, is a substrate of bacterial methylthioadenosine/S-adenosylhomocysteine (MTA/SAH) nucleosidase and a product inhibitor produced by radical SAM enzymes. 5′-dADO may be useful to study the specificity and distribution of radical S-adenosyl-L-methionine enzymes.

GSK321 is a potent and selective IDH1 mutant inhibitor. GSK321 potently inhibited intracellular 2-HG production in HT-1080 cells, with a half-maximal effective concentration (EC50) of 85 nM by LC/MS/MS analysis. The inhibition of mutant IDH1 by GSK321 overcomes the pathognomonic differentiation block of AML cells and induces myeloid differentiation of IDH1 mutant cells at the level of leukemic blasts and more stem-like cells.

Perillyl alcohol, or POH, is a naturally occurring monocyclic terpenes derived from the mevalonate pathway in plants. Perillyl alcohol can be found in the essential oils of various botanicals, such as lavender, lemongrass, sage, and peppermint. It has a number of manufacturing, household, and medical applications. For example, perillyl alcohol may be used as an ingredient in cleaning products and cosmetics, and it has shown promise for inhalation therapy of patients with brain cancer.

FR-122047 is a potent and selective cyclooxygenase-1 (COX-1) inhibitor (IC50 values are 0.028 and 65 μM for COX-1 and COX-2 respectively). FR122047 treatment led to a distinct suppression of cell growth in MCF-7 cells. FR122047 may have an anti-cancer potential in breast cancer.

GNF-1331 is a Potent, Selective, and Orally Bioavailable Porcupine Inhibitor (IC50 = 12 nM). Blockade of aberrant Wnt signaling is an attractive therapeutic approach in multiple cancers. Wnt signaling is tightly controlled during cellular proliferation, differentiation, and embryonic morphogenesis. Aberrant activation of this pathway plays a critical role in a variety of cancers, such as cutaneous squamous cell carcinoma (SCC), breast cancer, and colorectal cancer.

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.

CRT0044876 is a potent BER inhibitor or DNA Base Excision Repair Pathway Inhibitor (APE1 IC50 - 3 microM). CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds, with accumulation of apurinic sites.

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.

JX-06 is a potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor (IC50 values are 28, 49 and 313 nM for PDK2, PDK1 and PDK3, respectively). JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. JX06, as a selective covalent inhibitor of PDK1 in cells, forms a disulfide bond with the thiol group of a conserved cysteine residue (C240) based on recognition of a hydrophobic pocket adjacent to the ATP pocket of the PDK1 enzyme.

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.

BAY-598 R-isomer is the R-isomer of BAY589. BAY-598 R-isomer may be used as a reference compound. BAY-598 is a potent, peptide-competitive chemical probe for SMYD2. BAY-598 has a unique chemotype relative to the current SMYD2 chemical probe LLY-507. BAY-598 inhibits in vitro methylation of p53K370 with IC50 = 27 nM and has more than 100-fold selectivity over other histone methyltransferases and other non-epigenetic targets. BAY-598 inhibits the methylation of p53K370 in cells with IC50 < 1 μM. (Further to this, BAY-598 has properties that are compatible with in vivo experiments.) A control compound, BAY-369, has also been developed. BAY-369 inhibits the in vitro methylation of p53K370 with IC50 > 70 micromolar.

GSK-319347A is a potent and selective IKKε inhibitor (pIC50 = 7.4). GSK-319347A has a highly encouraging wider selectivity profile, including selectivity within the IKK kinase family.

eCF-309 is a potent mTOR inhibitor (IC50 = 15 nM).

9-hydroxyellipticine, also known as IGIG 929 and LS133324, is a potent cytotoxic and antitumor agent. Structurally, 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine. The hydroxy group in 9-hydroxyellipticines increases the apparent affinity for DNA, stabilisation of toposiomerase II-DNA cleavable complex, oxidation to reactive quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines.

OXA-01 is an inhibitor of both mTORC1 and mTORC2 (IC50s = 11 and 29 nM, respectively). OXA-01 targeted both mTORC1 and mTORC2 signaling in vitro and in vivo. OXA-01 reduced VEGF production in tumors in a manner associated with decreased vessel sprouting but little vascular regression.

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.

GSK-2250665A is a Itk inhibitor (pKi = 9.2).

Reticulol is an isocoumarin derivative produced by certain species of Streptomyces that inhibits cAMP phosphodiesterase (IC50 = 41 μM). Reticulol was isolated from the culture broth of the strain Streptoverticillium sp. NA-4803. Recticulol (M.W. 222.2) exhibited a potent in vitro cytotoxicity against A427, a human lung tumor cell line, and B16F10, a mouse melanoma cell line.

BIF-44, also known as 4-Phenoxyphenol and Hydroquinone monophenyl ether, is a sensitizer of BCL-2-associated X protein (BAX) activation by binding to a pocket formed by the junction of the α3-α4 and α5-α6 hairpins. BIF-44 enhances BAX activity.

CMP3a is a NEK2 kinase inhibitor. CMP3a efficiently attenuated GBM growth in a mouse model and exhibited a synergistic effect with radiotherapy. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2.

Trichostatin A S-isomer, also known as (-)-Trichostatin A, is the s-isomer of Trichostatin A. Trichostatin A has R-configuration structure, which is a HDAC inhibitor. Trichostatin A is a member of a larger class of histone deacetylase inhibitors (HDIs or HDACIs) that have a broad spectrum of epigenetic activities. TSA inhibits HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM.

CRT-0066854 is a PKCι and PKCζ inhibitor. CRT0066854, was able to restore polarized morphogenesis in the dysplastic H-Ras spheroids. These results show that tightly regulated PKCι is required for normal-polarized morphogenesis in mammalian cells and that H-Ras and ErbB2 cooperate with PKCι for loss of polarization and dysplasia. The identification of a PKCι inhibitor that can restore polarized morphogenesis has implications for the treatment of Ras and ErbB2 driven malignancies.

TCJL-37 is a potent TYK2 inhibitor.

D-Erythrose is an antitumor agent. D-Erythrose inhibits tumor growth in mice (in vivo). It is used to study the mechanisms of organic micro spherule formation and Maillard (glycation) reactions. D-erythrose significantly reduced the weight of the intraperitoneal tumor by 69.1%, markedly inhibited the development of ascites and increased tumor cell apoptosis, without any observed toxic effects. D-erythrose possesses antitumor activity against colon cancer.

BMS-605541 is a potent, orally active and selective VEGFR-2 inhibitor.

PSMA617-TCMC is a derivative of PSMA-617 with structure modification, in which the caroboxy groups in DOTA ring is replaced by TCMC macrocycle. PSMA-617 is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer,. PSMA-617 originally was developed at the German Cancer Research Center and the Heidelberg University Hospital. ABX held the exclusive license to bring the treatment, which targets prostate-specific membrane antigen (PSMA), through early clinical development.

MDK3627, also known as Mutant EGFR inhibitor, is a selective and potent Mutated EGFR inhibitor(L858R activating mutant,

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.

FM19G11 is an inhibitor of Hypoxia Inducible Factors α (HIFα), reported to affect self-renewal and differentiation of stem cells. Hypoxia-inducible factors (HIFs) are transcription factors that respond to changes in available oxygen in the cellular environment. Among other functions (like angiogenesis), HIFα proteins affect the self-renewal and the differentiation processes of stem cells. FM19G11 inhibits the HIFα proteins that repress the target genes of the two α subunits, in various tumor cell lines as well as in adult and embryonic stem cell (ESC) models.

STX140 is a bis-sulfamate derivative of the endogenous steroid 2-methoxyestradiol, has shown promising anticancer potency both in vitro and in vivo, with excellent bioavailability. STX140 is efficacious in vitro and in vivo in taxane-resistant breast carcinoma cells. STX140 causes apoptosis via the intrinsic mitochondrial pathway and down-regulate survivin and XIAP expression in ovarian and prostate cancer cells.

NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays.

GSK2807 is a potent and selective, SAM-competitive inhibitor of SMYD3 (Ki = 14 nM). GSK2807 bridges the gap between the SAM-binding pocket and the substrate lysine tunnel of SMYD3. GSK2807 may be useful for cancer treatment.

MUN21754, also known as JAK/HDAC-IN-1, is a potent and selective dual JAK2/HDAC inhibitor, MUN21754 exhibits antiproliferative and proapoptotic activities in several hematological cell lines. MUN21754 has CAS#2284621-75-4 and inchi key MTOQNLGMTJOJOF-UHFFFAOYSA-N. This product has no formal name. For the convenience of communication, we name it MUN21754. The 3 letters from its inch key and last 5 digit CAS# was used for name.

GSK3368715, aslo known as EPZ019997, is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell growth inhibition when combined with GSK3368715. Interestingly, deletion of the methylthioadenosine phosphorylase gene (MTAP) results in accumulation of the metabolite 2-methylthioadenosine, an endogenous inhibitor of PRMT5, and correlates with sensitivity to GSK3368715 in cell lines.

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.

LYN55979, also known as docetaxel-succinic-NHS ester, is a docetaxel derivative with an NHS ester bridged by a succinic linker. The NHS ester group of this molecule can effectively react with amino- or hydroxy- group to form conjugate product. LYN55979 is a useful agent to make docetaxel bio-conjugates. LYN55979 has CAS#960155-97-9. According to Hodoodo Chemical Nomenclature, we name it as LYN55979 for the convenience of scientific communications.

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.

BI-6C9 is an inhibitor of tBid (Kd = 20 μM).

Dicloxacillin sodium is an oral semisynthetic isoxazolyl antistaphylococcal penicillin. Most active of the isoxazolyl antistaphylococcal penicillins. Stable against penicillinase and active against many of the penicillinase-producing strains of Staphylococcus aureus. Clinical uses include skin and soft-tissue, bone and joint, respiratory tract, and urinary tract infections.

Haloperidol decanoate is a typical antipsychotic drug used as maintenance therapy for schizophrenia and mood disorders formulated as an ester for intramuscular injection.

Prosulfocarb is a widely used thiocarbamate herbicide in winter cereals.

Lorcainide hydrochloride is a antiarrhythmic agent with local anaesthetic activity. The antiarrhythmic actions of lorcainide are mediated by an impairment of fast sodium conductance. Pharmacologically, this drug appears effective in suppressing reentry phenomena and ectopic pacemaker activity, especially in the ventricles.

R-18986 is a biochemical.

Butylate is a thiocarbamate herbicide.

5-Hydroxymebendazole is a biochemical.

Cycloate is a herbicide. Cycloate inhibits the biosynthesis of very-long-chain fatty acids, the essential constituents of plant waxes and suberin. Fatty acids also serve as precursors of aliphatic carbon chains in resorcinolic lipids, which play a fundamental role in the plant defence system against fungal pathogens.

Fluanisone is a typical antipsychotic and sedative of the butyrophenone chemical class. It is used in the treatment of schizophrenia and mania. It is also a component (along with fentanyl) of the injectable veterinary formulation fentanyl/fluanisone (Hypnorm) where it is used for rodent analgesia during short surgical procedures.

Rebemide is a biochemical.

Carnidazole is an antiprotozoal drug of the nitroimidazole class used in veterinary medicine. It is used to treat Trichomonas infection.

Desethyl-etomidate is a biochemical.

Azaconazole is an agricultural fungicide. It is meant for controlling powdery mildew on crops and bean rust.

Pirimiphos-methyl (PMM) is a widely used organophosphorus pesticide that can be released into the atmosphere in gas and condensed phases.

Morazone is a nonsteroidal anti-inflammatory drug which is used as an analgesic. It produces phenmetrazine as a major metabolite and has been reported to have been abused as a recreational drug in the past.

Pirimiphos-ethyl is an organophosphorous pesticide.

Flurochloridone is a herbicide.

Spiramide is an antipsychotic that acts as a selective 5-HT2A, 5-HT1A, and D2 receptor antagonist. It has negligible affinity for the 5-HT2C receptor.

Spiperone is a antipsychotic that has been used to treat schizophrenia. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl? channels (CaCCs), thus a potential target for therapy of cystic fibrosis.

Loperamide oxide is a prodrug of the effective antidiarrheal loperamide.

Loreclezole is an anticonvulsant and antiepileptic compound.

Napropamide belongs to the amide herbicide family and widely used to control weeds in farmland.

Picolinamidoxime is a biochemical.

Rabeprazole thioether is an active metabolite of rabeprazole, a proton pump inhibitor.

Zilpaterol hydrochloride isa β-adrenergic receptor (AR) agonist. It is used to increase the size of cattle and the efficiency of feeding them.

Dihydrozeatin is a plant cytokinin. It is used in agriculture to make plants grow larger.

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

Propiconazole is an agricultural pesticide undergoing evaluation by the U.S. Environmental Protection Agency's Endocrine Disruptor Screening Program.

Padimate O is a UVB absorber. It is a major ingredient in sunscreens.

Rugulosin (RUG) is bis-anthraquinoid pigment produced by fungi such as Penicillium rugulosum Thom, P. tardum and others

Diatrizoate Sodium is an X-ray contrast agent. Diatrizoate sodium blocks X-rays which lets body structures with iodine to be delineated in comparison to the structures that do not have iodine. This is used as a diagnostic aid in angiography, urography and radiography.

Bromadiolone is a anticoagulant rodenticide, has been extensively used worldwide for the field control of rodents.

Ramiprilat is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.

Novolimus is a macrocyclic lactone with anti-proliferative properties, has a similar efficacy to currently available agents but it requires a lower dose and is therefore conceivably safer to use.

Umirolimus is a sirolimus derivative from a biodegradable polylactic acid polymer; it possesses enhanced anti-inflammatory and antiproliferative activity with an improved pharmacokinetic profile.

Coumachlor is a first genereation anticoagulant rodenticide which blocks formation of prothrombin and inhibits blood coagulation causing death by internal haemorrhage.

Coumafuryl is a anticoagulant rodenticide.

Coumatetralyl is an anticoagulant of the 4-hydroxycoumarin vitamin K antagonist type used as a rodenticide.

Pipemidic acid is a therapeutic agent for urinary tract infections. It is a member of the pyridopyrimidine class of antibacterials

Ofurace is a fungicide.

Clethodim is a acetyl-coenzyme A carboxylase (ACCase)-inhibiting cyclohexanedione herbicide used to control grass weeds infesting dicot crops.

Rebamipide exerts a mucosal-protective effect, mediated through several mechanisms. It is a routine drug for the treatment of gastritis in a clinical setting.

Oxyphenisatine is a laxative. Long-term use is associated with liver damage.

Fomesafen is a diphenyl ether herbicide that has an important role in the removal of broadleaf weeds in bean and fruit tree fields. It degrades slowly in soils and has been linked to crop damage.

Thifensulfuron-methyl is a sulfonylurea (SU) herbicide.

Ronnel is an organophosphate pesticide with growth-promoting properties.

Trietazine is a herbicide.

Maneb is an fungicide widely used to control fungal diseases on crops, fruits, and vegetables.

Diatrizoate meglumine is the meglumine salt form of diatrizoate, an organic, iodinated, radiopaque X-ray contrast medium used in diagnostic radiography.

Propagermanium is an organometallic compound of germanium that has been used as a therapeutic agent against chronic hepatitis B in Japan.

Unoprostone isopropyl is a prostanoid and synthetic docosanoid approved for the treatment of open-angle glaucoma and ocular hypertension.

Retrorsine is a hepatotoxic pyrrolizidine alkaloid present in plants of the Senecio genus.

Triazamate is a dimethylcarbamate insecticide.

Halofenozide is a non-steroidal ecdysone agonist. It is used as a potent insecticide.

Oxyfluorfen is a herbicide of the nitrodiphenyl ether class. It is being used to control annual and perennial broad-leaved weeds and sedges in a variety of field crops.

Convallatoxin is a cardiac glycoside extracted from Convallaria majalis. It is mainly used for acute and chronic heart failure.

Iprobenfos (IBP) is an organophosphorus pesticide.

Sisomicin is an aminoglycoside antibiotic that is highly active against staphylococci.

Anilofos is a widely used thionoorganophosphate herbicide. It is used for pre-emergence and early post-emergence control annual grass weeds and sedges in transplanted rice crops.

Piperophos is an organophosphate and anti-androgenic compound.

Fenarimol is a pyrimidine-type fungicide that exhibits potent inhibitory activity against BR biosynthesis.

Rimorphin is an opioid peptide derived from prodynorphin and a κ-opioid receptor agonists

Gamma cyclodextrin is a biochemical found in some foods.

Oxadixyl is a fungicide.

Temocaprilat is the diacid of temocapril and an angiotensin-converting enzyme inhibitor.

Fenpropidin is a morpholine class antifungal that is a specific inhibitor of sterol 14-reductase.

Isoacitretin is an oral retinoid effective in the treatment of psoriasis.

Amorolfine is commonly available in the form of a nail lacquer. It is a topical application used to treat fungal nail infections.

Pyrifenox is an azole inhibitor and pesticide.

Propaquizafop is a phenoxyisopropionic acid derivative and is used as a herbicide.

Iomazenil is an antagonist and partial inverse agonist of benzodiazepine and a potential treatment for alcohol abuse.