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GSK2830371

品牌
Sigma-Aldrich
CAS
1404456-53-6
货号
SML1048
规格纯度
≥98% (HPLC)
价格
1117.23 *本价格含增值税费
促销
服务
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数量
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半岛bd体育手机客户端 名称:
1404456-53-6
GSK2830371
5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide
(S)-5-(((5-Chloro-2-methylpyridin-3-yl)amino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

包装

5, 25 mg in glass bottle

生化/生理作用

GSK2830371 is an orally active allosteric inhibitor of wild-type p53-induced phosphatase (Wip1, also known as PPM1D/ PP2Cδ), an oncogenic type 2C serine/threonine phosphatase that negatively regulates key proteins in the DNA damage–response pathway. GSK2830371 is selective for Wip1 with an IC50of 6 nM against Wip1 compared to >10 μM IC50for PPM1A & PPM1K, and >30 μM IC50for 22 other phosphatases tested. GSK2830371 is believed to interact with the flap subdomain located near the Wip1 catalytic site, a feature that distinguishes Wip1 from other members of the protein phosphatase 2C (PP2C) family. GSK2830371 increased phosphorylation of Wip1 substrates and caused growth inhibition in both hematopoietic tumor cell lines and Wip1-amplified breast tumor cells harboring wild-type TP53.
GSK2830371 prevents the development of neuroblastoma by stimulating cell death mediated by Chk2 (checkpoint kinase 2)/p53. In neuroblastoma (NB) cell lines, GSK2830371 increased the cytotoxicity stimulated by doxorubicin- (Dox) and etoposide- (VP-16). It also blocks the capability of a subset of NB cells in multiplication and colony formation.

基本信息

经验(实验)分子式 C23H29ClN4O2S
分子量 461.02
NACRES NA.77

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 powder
颜色 white to beige
溶解性 DMSO: 20 mg/mL, clear
储存温度 2-8℃

安全信息

储存分类代码 13 - Non Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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