Biochem/physiol Actions
An apoptosis inducer that selectively targets the anti-apoptotic Bcl-2 family member Bcl-XL with high affinity.
WEHI-539 is an apoptosis inducer that selectively targets the anti-apoptotic Bcl-2 family member Bcl-XL with high affinity (KD = 0.6 nM; 500-fold over Bcl-2 and 400-fold over Bcl-W, Mcl-1 and A1) in a manner distinct from that of ABT-737. WEHI blocks Bcl-XL from targeting the BH3 domain of the pro-apoptotic family member Bim with high potency (IC50 = 1.1 nM), exhibiting no inhibitory potency against Mcl-1-BimBH3 interaction (IC50 >10 μM). WEHI-539 is shown to induce apoptosis in human and murine cultures by selectively antagonizing Bcl-XL prosurvival activity (EC50 <10 nM/Mcl-1-knockout MEF, <0.5 nM/mouse platelets, and <32 nM/human platelets).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | faint yellow to dark orange |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | [s]1c(nc(c1CCCOc6ccc(cc6)CN)C(=O)O)c2cc3c(cc2)CCC=C3NNc4[s]c5c(n4)cccc5 |
| InChI | 1S/C31H29N5O3S2/c32-18-19-10-14-22(15-11-19)39-16-4-9-27-28(30(37)38)34-29(40-27)21-13-12-20-5-3-7-24(23(20)17-21)35-36-31-33-25-6-1-2-8-26(25)41-31/h1-2,6-8,10-15,17,35H,3-5,9,16,18,32H2,(H,33,36)(H,37,38) |
| InChI key | BDQRJRWAPLGIFF-UHFFFAOYSA-N |
