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WEHI-539 hydrochloride

HY-15607A

(WEHI539 hydrochloride; WEHI 539 hydrochloride)

WEHI-539 hydrochloride

WEHI-539 hydrochloride Chemical Structure

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).

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $248 In-stock
5 mg $182 In-stock
10 mg $223 In-stock
50 mg $870 In-stock
100 mg Get quote
200 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €243 In-stock
5 mg €178 In-stock
10 mg €219 In-stock
50 mg €853 In-stock
100 mg Get quote
200 mg Get quote

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Product name: WEHI-539 hydrochloride
Cat. No.: HY-15607A

WEHI-539 hydrochloride Data Sheet

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    Purity: 98.66%

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Biological Activity of WEHI-539 hydrochloride

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).
IC50 Value: 1.1 nM (BCL-XL) [1]
Target: Bcl-2 Family
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 killing of platelets purified from mice or humans in culture.
 

Chemical Information

M.Wt 620.18 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C31H30ClN5O3S2
CAS No
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.6124 mL 8.0622 mL 16.1244 mL
5 mM 0.3225 mL 1.6124 mL 3.2249 mL
10 mM 0.1612 mL 0.8062 mL 1.6124 mL

References on WEHI-539 hydrochloride

Other Forms

  • WEHI-539

    CAS No.: 1431866-33-9 Get quote

Inhibitor Kit

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