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WEHI-539 hydrochloride

Catalog No.: 6111405
Cas No.:
Purity : 98% 
6111405 - WEHI-539 hydrochloride

Catalog number : 6111405

CAS number :

Molecular Formula : C31H30ClN5O3S2 

Molecular Weight : 620.18 

Iupac Chemical Name : WEHI-539 hydrochloride 

Smile : C[Si](C)(C)CSCCl

InChiKey : IKWIERSJEROYFH-UHFFFAOYSA-N

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SynonymsWEHI539 hydrochloride; WEHI 539 hydrochloride 
Molecular FormulaC31H30ClN5O3S2 
Molecular Weight620.18 
Appearancecrystalline solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
SmileC[Si](C)(C)CSCCl
InChiKeyIKWIERSJEROYFH-UHFFFAOYSA-N
InChiInChI=1S/C5H13ClSSi/c1-8(2,3)5-7-4-6/h4-5H2,1-3H3
MDLMFCD17013410
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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.

 

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