GDC-0152

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

Cat. No. ：BCP08767CAS No. ：873652-48-3Purity：98%

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CAS No.	873652-48-3	Cat. No.	BCP08767
Name	GDC-0152
Synonyms	GDC0152; GDC 0152;
SMILES
Chemical Name
Formula	C25H34N6O3S	M. Wt	498.64
Purity	98%	Storage	Store at 4-8°C
Description	in vitro:GDC-0152 can block protein?protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. In melanoma SK-MEL28 cells, the endogenous association of ML-IAP and Smac is effectively also abolished by GDC-0152. GDC-0152 lead to a decrease in cell viability in the MDA-MB-231 breast cancer cell line, while having no effect on normal human mammary epithelial cells (HMEC). GDC-0152 is found to activate caspases 3 and 7 in a dose- and time-dependent manner. GDC-0152 is shown to induce rapid degradation of cIAP1 in A2058 melanoma cells. It effectively induces degradation of cIAP1 at concentrations as low as 10 nM, consistent with its affinity for cIAP1. In vivo: GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes.