TH-302 is a hypoxia-activated prodrug consisting of a 2-nitroimidazole phosphoramidate conjugate with potential antineoplastic activity. The 2-nitroimidazole moiety of hypoxia-activated prodrug TH-302 acts as a hypoxic trigger, releasing the DNA-alkylating dibromo isophosphoramide mustard moiety within hypoxic regions of tumors. Normoxic tissues may be spared due to the hypoxia-specific activity of this agent, potentially reducing systemic toxicity.

 June 21, 2017

prudect name : TH-302 is a hypoxia-activated prodrug consisting of a 2-nitroimidazole phosphoramidate conjugate with potential antineoplastic activity. The 2-nitroimidazole moiety of hypoxia-activated prodrug TH-302 acts as a hypoxic trigger,…

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SRT1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 ¦ÌM and maximum activation = 781%) versus the closest sirtuin homologues, SIRT2 and SIRT3£¬(SIRT2: EC1.5 = 37 ¦ÌM£»SIRT3: EC1.5 > 300 ¦ÌM). This agent binds to the SIRT1 enzyme-peptide substrate complex at an allosteric site amino-terminal to the catalytic domain and lower the Michaelis constant for acetylated substrates.

prudect name : SRT1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 ¦ÌM and maximum activation = 781%) versus the closest sirtuin homologues, SIRT2 and SIRT3£¬(SIRT2: EC1.5 =…

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Japan¡¯s Kissei Pharmaceutical Company invented ¦Á1-receptor antagonist for the treatment of benign prostatic hyperplasia (BPH), or hypertrophy-related symptoms

prudect name : Japan¡¯s Kissei Pharmaceutical Company invented ¦Á1-receptor antagonist for the treatment of benign prostatic hyperplasia (BPH), or hypertrophy-related symptomsSilodosin Synonyms: CAS NO: 160970-54-7Molecular Formula: C25H32F3N3O4Molecular Weight: 495.53Purity: 99%Solubility:…

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SNX-2112 is a potent synthetic heat shock protein 90 inhibitor with an IC50 of 0.92 ¦ÌM for K562 cells. The heat shock protein 90 (Hsp90) chaperone not only regulates the conformational maturation but also stables the structures of oncogenic kinases as well as transcription factors. SNX-2112 is an active metabolite of the compounds SNX-5542. SNX-2112 is rapidly transformed form SNX-5542 after administration. In a panel of tumor cell lines, SNX-2112 degraded HER2 and mutant epidermal growth factor receptor and inhibited extracellular signal-modulated kinase and Akt activation.SNX-2112 inducen a Rb-dependent G1 arrest with subsequent apoptosis. which accumulates in tumors relative to normal tissues.

prudect name : SNX-2112 is a potent synthetic heat shock protein 90 inhibitor with an IC50 of 0.92 ¦ÌM for K562 cells. The heat shock protein 90 (Hsp90) chaperone not…

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AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways.,

prudect name : AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through…

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Biological Activity: Orally active, selective 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, ¦Á1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 ¦ÌM).

prudect name : Biological Activity: Orally active, selective 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at...

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SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription.

prudect name : SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has…

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SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.

prudect name : SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.SW033291 Synonyms: CAS NO: 459147-39-8Molecular Formula: C21H20N2OS3Molecular Weight:…

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prudect name : sitafloxacinSynonyms: CAS NO: 127254-12-0Molecular Formula: C19H18ClF2N3O3Molecular Weight: 409.81Purity: ≥99%Solubility: Storage: −20°C

prudect name : sitafloxacin Synonyms: CAS NO: 127254-12-0Molecular Formula: C19H18ClF2N3O3Molecular Weight: 409.81Purity: ≥99%Solubility: Storage: −20°C 2 years web site: www.medchemexpress.com

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SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2 and PDGFR at rate of 97%, 65% and 55%, respectively, at concentration of 10 ¦ÌM in biochemical kinase assays.

prudect name : SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2 and PDGFR at rate of 97%, 65% and 55%, respectively, at concentration of 10 ¦ÌM in…

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