位置:首页 > 品牌 > Sigma-Aldrich >

STAT3/STAT5 Dual Inhibitor, SH-4-54-Calbiochem

品牌
Sigma-Aldrich
货号
5.09105
规格纯度
A cell-permeable BP-1-102 analog that targets STAT3 and STAT5 with comparable affinity.
参考价格
2579.1 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable, salicyclic-to-benzoic acid-substituted BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity (koff/kon = KD = 300 and 464 nM, respectively) and is 4-fold more potent in competing against phosphopeptide for binding to SH2 domain of STAT3 over STAT1 (Ki = 23.5 and 92.3 µM, respectively; [phosphopeptide] = 10 nM), exhibiting little potency against the kinase activity of upstream kinases (Akt1, Erk1, JAK1/2, c-Src) or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice (Conc in brain = 313 nM 30 min post 10 mg/kg i.p. dosing) and effectively inhibit BT73 glioma proliferation in xenografted murine brain via apoptosis induction (10 doses: 10 mg/kg i.p., 4 d on/ 3 d off) in vivo.
A cell-permeable BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity and is 4-fold more potent in competing against phosphopeptide for binding SH2 domain of STAT3 over STAT1, exhibiting little potency against upstream kinases or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) in cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice and effectively inhibit BT73 glioma proliferation in xenografted murine brain (10 mg/kg/d via i.p.; 4 d on/ 3 d off) in vivo.

生化/生理作用

Cell permeable: yes
Secondary Target
STAT5
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

Haftchenary, S., et al. 2013. ACS Med. Chem. Lett.4, In press.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C29H27F5N2O5S
分子量610.59

产品性质

质量水平100
测定≥94% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 100 mg/mL
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

推荐产品
| 首页 | 联系我们 | 会员服务 | 广告服务 | 友情链接 |
版权所有 CopyRight © 2008-2024 粤ICP备08119708号