现货,Obatoclax (GX15-070),CAS号:803712-79-0,美国进口,细胞凋亡(Apoptosis) ,Bcl-2,Bcl-2 抑制剂和化合物

信号转导通路: 细胞凋亡(Apoptosis) >> Bcl-2 >> Bcl-2 抑制剂和化合物 >> Obatoclax mesylate (GX15-070)http://selleck.cn/obatoclax-mesylate-S1057.html

技术数据:

分子量(MW): 413.49

化学式:

C20H19N3O.CH4O3S

 

溶解度: DMSO ≥83mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: 99%

稳定性: at -20℃ 2 years

CAS号: 803712-79-0

生物活性

 

 

Endogenous proteins that contain Bcl-2 homology domain-3 (BH3), bind to antiapoptotic Bcl-2-family members, and promote the release of Bax and Bak ,which permeabilize the outer mitochondrial membrane to release apoptogenic factors[1]

Specific apoptosis was induced at 250 nM obatoclax mesylate (16.04 %) and increased in a dose-dependent manner up to the highest dose tested (10 µM, 73.48 %). The average IC50 for the seven AML patient samples tested was 3.59 µM. [2]

Obatoclax mesylate (GX15-070) has been reported to similarly antagonize all antiapoptotic Bcl-2 family proteins (average IC50=3 µM), including Mcl-1 (IC50=2.9 µM) and Bfl-1 (IC50=5 µM) [3]

 

 

 

参考文献

Mitochondria and Apoptosis Douglas R. Green and John C. Reed SCIENCE 28 AUGUST 1998;281:1309-1312

Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax) Julie Watt, Rooha Contractor, et al. Cancer Res 2008;68:3413-3420

Comparison of chemical inhibitors of antiapoptotic Bcl-2-family proteins Cell Death and Differentiation 2006;13:1419–1421

 

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