Name: GDC-0152
Price: 297.00 USD

- Overview
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    Background
    
    GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins, including ML-IAP, XIAP, cIAP1 and cIAP2, that binds to the BIR domain of ML-IAP and the BIR3 domains of XIAP, cIAP1 and cIAP2 with values of inhibition constant Ki of 14 nM, 28 nM, 17 nM and 43 nM respectively. GDC-0152 potentially inhibits tumor growth of breast cancer by promoting cIAP1 degradation and inducing caspase-3/7 activation which result in the decreasing of cell viability of breast cancer cells with normal epithelial cells unaffected. In recent studies, GDC-0152 shows its ability to disrupt the binding of XIAP to caspase-9 and the association of ML-IAP, cIAP1 and cIAP2 with Smac in HEK293T cells.
- Properties
  - Categories
    
    IAP antagonist, potent amd samll-molecule
    
    Alternative Name
    
    GDC0152, GDC 0152; (2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide
    
    CAS Number
    
    873652-48-3
    
    Molecular Formula
    
    C25H34N6O3S
    
    Molecular Weight
    
    498.64
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥24.95 mg/mL in DMSO; insoluble in H2O; ≥50.6 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(C(=O)NC(C1CCCCC1)C(=O)N2CCCC2C(=O)NC3=C(N=NS3)C4=CC=CC=C4)NC
    
    * For Research Use Only
- Reference
  - 1. Jung H, Leal-Ekman JS, et al. "Atg14 protects the intestinal epithelium from TNF-triggered villus atrophy." Autophagy. 2019 Mar 20:1-12. PMID:30894050
    2. Rosner A, Kravchenko O, et al. "IAP genes partake weighty roles in the astogeny and whole body regeneration in the colonial urochordate Botryllus schlosseri." Dev Biol. 2018 Oct 30. pii: S0012-1606(17)30904-1. PMID:30385275