WEHI539

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP14752CAS No. ：1431866-33-9Purity：98%

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CAS No.	1431866-33-9	Cat. No.	BCP14752
Name	WEHI539
Synonyms	WEHI-539;WEHI 539;
SMILES
Chemical Name
Formula	C31H29N5O3S2	M. Wt	583.72
Purity	98%	Storage	Store at 4-8°C
Description	The prosurvival BCL-2 family protein BCL-XL is often overexpressed in solid tumors and renders malignant tumor cells resistant to anticancer therapeutics. The optimized compound, 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 k