化合物BMS582949 T6789

Product Introduction
Bioactivity


英文名: BMS582949

描述: BMS582949 (PS540446) 是一种有效的选择性 p38 丝裂原活化蛋白激酶(p38 MAPK) 抑制剂，IC50 为 13 nM，抑制 p38 激酶活性和 p38 活化。

激酶实验: Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography.

体外活性: BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop[2].

体内活性: 小鼠对BMS-582949的清除率为4.4 mL/min/kg。口服剂量10 mg/kg时，小鼠BMS-582949的AUC0-8 h为75.5 μMh。在小鼠和大鼠中，BMS-582949展示出90%和60%的口服生物利用度[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 75 mg/mL (184.5 mM)


关键字: BMS582949 | PS-540446 | PS 540446

相关产品: Farrerol | Esculin | Dehydroglyasperin C | p38 Kinase inhibitor 4 | Hesperetin | Dehydroglyasperin D | Sesamolin | Isochamaejasmine | TAK-715 | SB 239063

相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Pyroptosis Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Cancer Cell Differentiation Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Pancreatic Cancer Compound Library

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