GDC-0152

• CAT Number: I005261
• CAS Number: 873652-48-3
• Molecular Formula: C25H34N6O3S
• Molecular Weight: 498.64
• Purity: ≥95%
• Synonyms: (2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide
• Target: IAP
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 28/14/17/43 nM(Ki, XIAP/ML-IAP/cIAP1/cIAP2)
• InChI: 1S/C25H34N6O3S/c1-16(26-2)22(32)27-21(18-12-7-4-8-13-18)25(34)31-15-9-14-19(31)23(33)28-24-20(29-30-35-24)17-10-5-3-6-11-17/h3,5-6,10-11,16,18-19,21,26H,4,7-9,12-15H2,1-2H3,(H,27,32)(H,28,33)/t16-,19-,21-/m0/s1
• InChIKey: WZRFLSDVFPIXOV-LRQRDZAKSA-N
• SMILES: C[C@@H](C(=O)N[C@@H](C1CCCCC1)C(=O)N2CCC[C@H]2C(=O)NC3=C(N=NS3)C4=CC=CC=C4)NC

GDC-0152 (CAT: I005261) is a potent inhibitor of apoptosis proteins (IAPs), specifically binding to the BIR3 domains of XIAP, ML-IAP, cIAP1, and cIAP2 with Ki values ranging from 14 to 43 nM. In vitro studies demonstrate that GDC-0152 disrupts protein-protein interactions involving IAPs and pro-apoptotic molecules, leading to decreased cell viability and activation of caspases. GDC-0152 induces degradation of cIAP1 in melanoma cells and shows selectivity for cancer cells over normal cells. In vivo, GDC-0152 exhibits moderate hepatic clearance and plasma protein binding across multiple species, with pharmacokinetic parameters including a Cmax of 53.7 μM and AUC of 203.5 h-μM. These findings highlight the potential of GDC-0152 as an IAP inhibitor for targeted cancer therapy.