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BMS582949
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS582949图片
CAS NO:623152-17-0
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PS540446
BMS-582949
BMS 582949
产品介绍
BMS582949 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。

产品描述

BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38.

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

The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM?h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1].

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.

Cas No.

623152-17-0

分子式

C22H26N6O2

分子量

406.49

别名

PS540446;BMS-582949;BMS 582949

储存和溶解度

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:75 mg/mL (184.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years