An inhibitor of IAPs
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

GDC-0152

Item No. 17810

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(4-phenyl-1,2,3-thiadiazol-5-yl)-L-prolinamide
CAS Number
873652-48-3
Molecular Formula
C25H34N6O3S
Formula Weight
498.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
230, 255, 293 nm
SMILES
O=C(N[C@@H](C1CCCCC1)C(N2CCC[C@H]2C(NC3=C(C4=CC=CC=C4)N=NS3)=O)=O)[C@@H](NC)C
InChi Code
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
InChi Key
WZRFLSDVFPIXOV-LRQRDZAKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $49

    Add

    5 mg

    $202

    Add

    10 mg

    $329

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    Product Description

    GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively).1 GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.1,2 It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.1 GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.3 In dogs and rats, but not humans, this leads to a pronounced inflammatory response.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Flygare, J.A., Beresini, M., Budha, N., et al. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). J. Med. Chem. 55(9), 4101-4113 (2012).

    2. Hu, R., Li, J., Liu, Z., et al. GDC-0152 induces apoptosis through down-regulation of IAPs in human leukemia cells and inhibition of PI3K/Akt signaling pathway. Tumour Biol. 36(2), 577-584 (2015).

    3. Erickson, R.I., Tarrant, J., Cain, G., et al. Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-α pharmacology. Toxicol. Sci. 131(1), 247-258 (2013).