A potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28

GDC-0152 – 1 mg

Brand:
Cayman
CAS:
873652-48-3
Storage:
-20
UN-No:
Non-Hazardous - /

Inhibitor of apoptosis proteins (IAPs), which block various signaling pathways leading to apoptotic cell death, are commonly over-expressed in cancer cells.{9448} 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).{29254} GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.{29254,29255} It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.{29254} GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.{29253} In dogs and rats, but not humans, this leads to a pronounced inflammatory response.{29253}  

 

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Description

A potent inhibitor of specific IAPs that binds baculovirus 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); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells

Formal name: N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(4-phenyl-1,2,3-thiadiazol-5-yl)-L-prolinamide

Synonyms: 

Molecular weight: 498.6

CAS: 873652-48-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation

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