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描述 | GDC-0152 disrupts protein−protein interactions involving IAP proteins and pro-apoptotic molecules. In HEK293T cells transiently transfected, GDC-0152 disrupts XIAP binding to partially processed caspase-9 and the association of ML-IAP, cIAP1, and cIAP2 with Smac. In SK-MEL28 melanoma cells, GDC-0152 effectively abolishes the endogenous association of ML-IAP and Smac. It reduces cell viability in MDA-MB-231 breast cancer cells but not in normal human mammary epithelial cells (HMEC). GDC-0152 activates caspases 3 and 7 in a dose- and time-dependent manner. Additionally, GDC-0152 induces rapid degradation of cIAP1 in A2058 melanoma cells, with effective degradation observed at concentrations as low as 10 nM, consistent with its affinity for cIAP1 [1]. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A2058 cells | Function assay | 15 mins | Induction of proteasomal degradation of cIAP1 in human A2058 cells after 15 mins by immunoblotting | 22413863 | |
HEK293T cells | 1-50 μM | Function assay | 2 h | Inhibition of Flag-tagged XIAP BIR3 domain binding to cIAP1 expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation | 22413863 |
MDA-MB-231 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescent assay | 22413863 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.01mL 0.40mL 0.20mL |
10.03mL 2.01mL 1.00mL |
20.05mL 4.01mL 2.01mL |
参考文献 |
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