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A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator with an EC50 of 0.8 ¦ÌM.A-769662 displays selectivity towards ¦Â1 subunit-containing heterotrimers. A-769662 not only inhibits fatty acid synthesis with an IC50 of 3.2 ¦ÌM but also decreases plasma glucose and triglyceride levels in vivo. The addition of A-769662 to mouse embryonic fibroblasts or primary mouse hepatocytes stimulates phosphorylation of acetyl-CoA carboxylase (ACC), effects that are completely abolished in AMPK-alpha1(-/-)alpha2(-/-) cells but not in TAK1(-/-) mouse embryonic fibroblasts. Phosphorylation of AMPK and ACC in response to A-769662 is also abolished in isolated mouse skeletal muscle lacking LKB1, a major upstream kinase for AMPK in this tissue. A-769662 directly prevents the alpha(1)-isoform of the Na(+)-K(+)-ATPase which is purified from rat and human kidney cells in vitro with IC50 of 57 ¦ÌM and 220 ¦ÌM, respectively. Suppression of the Na(+)-K(+)-ATPase by 100 ¦ÌM ouabain decreases sodium pump activity and cell surface abundance, similar to the effect of A769662 (A 769662; A-769662), without influencing the phosphorylation of AMPK and ACC

June 21, 2017

prudect name : A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator with an EC50 of 0.8 ¦ÌM.A-769662 displays selectivity towards ¦Â1 subunit-containing heterotrimers. A-769662 not only inhibits fatty…

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amsilarotene (TAC-101) is a retinobenzoic acid with potential antineoplastic activity. TAC-101 inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression.

prudect name : amsilarotene (TAC-101) is a retinobenzoic acid with potential antineoplastic activity. TAC-101 inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting…

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AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3beta and S6 ribosomal protein phosphorylation, and also causes growth inhibition in a range of human cancer cell lines as a single agent. Induction of apoptosis was detected by multiple methods in tumor cells following AT7867 treatment. Administration of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) to athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model caused inhibition of phosphorylation of downstream substrates of both AKT and p70S6K and induction of apoptosis, confirming the observations made in vitro. These doses of AT7867 also resulted in inhibition of human tumor growth in PTEN-deficient xenograft models. These data suggest that the novel strategy of AKT and p70S6K blockade may have therapeutic value and supports further evaluation of AT7867 as a single-agent anticancer strategy.

prudect name : AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small…

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AVL-292 is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM; >1400-fold selectivity over the other kinases assayed.

prudect name : AVL-292 is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM; >1400-fold selectivity over the other kinases assayed.AVL-292 Synonyms:…

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AZD5438 a potent cyclin-dependent kinase (cdk) 1, 2 and 9 inhibitor with IC50 of 16, 6 and 20 nM, respectively. AZD5438 exhibits antiproliferative activity in human tumor cell lines. AZD5438 blocks cell cycling at G2-M, S and G1 phases. AZD5438 reduces the proportion of actively cycling cells in vivo. In vitro, AZD5438 showed significant antiproliferative activity in human tumor cell lines (IC50 range, 0.2-1.7 ¦ÌM), causing inhibition of the phosphorylation of cdk substrates pRb, nucleolin, protein phosphatase 1a, and RNA polymerase II COOH-terminal domain and blocking cell cycling at G2-M, S, and G1 phases. In vivo, when orally administered at either 50 mg/kg twice daily or 75 mg/kg once daily, AZD5438 inhibited human tumor xenograft growth. In vivo, AZD5438 reduced the proportion of actively cycling cells.

prudect name : AZD5438 a potent cyclin-dependent kinase (cdk) 1, 2 and 9 inhibitor with IC50 of 16, 6 and 20 nM, respectively. AZD5438 exhibits antiproliferative activity in human tumor…

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AZD-3463 is a ALK/IGF1R inhibitor.

prudect name : AZD-3463 is a ALK/IGF1R inhibitor.AZD-3463 Synonyms: CAS NO: 1356962-20-3Molecular Formula: C24H25ClN6OMolecular Weight: 448.95Purity: 98% minSolubility: In DMSOStorage: -20°C 871700-17-3 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18498226

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prudect name : Atomoxetine hydrochlorideSynonyms: CAS NO: 82248-59-7Molecular Formula: C17H21NO.HClMolecular Weight: 291.82Purity: 99%Solubility: Storage: −20°C

prudect name : Atomoxetine hydrochloride Synonyms: CAS NO: 82248-59-7Molecular Formula: C17H21NO.HClMolecular Weight: 291.82Purity: 99%Solubility: Storage: −20°C 2 years 221244-14-0 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18498133

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prudect name : AgomelatineSynonyms: CAS NO: 138112-76-2Molecular Formula: C15H17NO2Molecular Weight: 243.30Purity: 99%Solubility: Storage: −20°C 2

prudect name : Agomelatine Synonyms: CAS NO: 138112-76-2Molecular Formula: C15H17NO2Molecular Weight: 243.30Purity: 99%Solubility: Storage: −20°C 2 years 1062368-24-4 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18498117

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Abacavir for human immunodeficiency virus (HIV) infection in antiretroviral combination therapy.

prudect name : Abacavir for human immunodeficiency virus (HIV) infection in antiretroviral combination therapy.Abacavir Synonyms: CAS NO: 136470-78-5Molecular Formula: C14H18N6OMolecular Weight: 286.34Purity: 99% minSolubility: Storage: −20°C 849217-68-1 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18498065

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Ascomycin (FK-520) is a variant of ascomyceticus from Streptomyces hygroscopicus isolated from fermentation secondary metabolites. Immunosuppressive activity is a non-polar macrolide.

prudect name : Ascomycin (FK-520) is a variant of ascomyceticus from Streptomyces hygroscopicus isolated from fermentation secondary metabolites. Immunosuppressive activity is a non-polar macrolide.Ascomycin Synonyms: CAS NO: 104987-12-4Molecular Formula: C43H69NO12Molecular…

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