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WEHI-539 hydrochloride 编号 : 6111405

化学信息

产品英文名称WEHI-539 hydrochloride
Iupac 化学名称WEHI-539 hydrochloride 
同义词WEHI539 hydrochloride; WEHI 539 hydrochloride 
英文同义词WEHI539 hydrochloride; WEHI 539 hydrochloride 
分子式C31H30ClN5O3S2 
分子量620.18 
SmileC[Si](C)(C)CSCCl
InChiKeyIKWIERSJEROYFH-UHFFFAOYSA-N
InChiInChI=1S/C5H13ClSSi/c1-8(2,3)5-7-4-6/h4-5H2,1-3H3
MDLMFCD17013410

技术数据

外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature as non-hazardous chemical. 
质量控制

产品详情

WEHI-539, has high affinity (subnanomolar) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. WEHI-539 has a high affinity for BCL-XL (IC50 = 1.1 nM). 

WEHI-539 interacts with residues in the P4 pocket and adopts a distinct binding mode compared to ABT-737. WEHI-539 induces apoptosis in MEFs only if they lack MCL-1 supports the notion that cell killing induced by WEHI-539 is due to direct inhibition of BCL-XL. Accordingly, restoring expression of MCL-1 in mcl-1 knockout cells renders them highly resistant to WEHI-539. WEHI-539 could only kill cells that contained BAK (Fig. 6b). This observation was confirmed in MEFs where both the amount and activity of MCL-1 were abrogated by expression of its natural and selective BH3-only ligand NOXA. Cytochrome c release and caspase-3 processing confirmed that WEHI-539 induces apoptosis in BAX-deficient MEF cells expressing BIM2A but not in their BAK-deficient counterparts. Remarkably, WEHI-539 efficiently triggered the killing of platelets purified from mice or humans in culture.

 

结构

6111405 - WEHI-539 hydrochloride

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