| 溶解性 | 25°C: DMSO |
| 存贮条件 | 储存温度-20°C |
| 生化机理 | Description:IC50 Value: 1.1 nM (BCL-XL) [1]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, 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. |
WEHI-539
WEHI-539 （订货以英文为准）
编号：W125716
CAS号：1431866-33-9
分子式：C31H29N5O3S2
分子量：583.72
| 产品名称 | WEHI-539 |
| 中文名称 | WEHI-539 |
| CAS号 | 1431866-33-9 |
| 分子式（M.F.） | C31H29N5O3S2 |
| 分子量（M.W.） | 583.72 |
| 储存条件 | -20°C储存 |
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