Preferred Label : Smac Mimetic GDC-0917;
NCIt synonyms : IAP Antagonist GDC-0917; SMAC/DIABLO Mimetic GDC-0917; L-Prolinamide, N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(2-(2-oxazolyl)-4-phenyl-5-thiazolyl)-;
NCIt related terms : GDC-0917;
NCIt definition : An orally available, monovalent mimetic of second mitochondrial-derived activator
of caspases (Smac/DIABLO) and inhibitor of IAPs (Inhibitor of Apoptosis Proteins)
with potential antineoplastic activity. Smac mimetic GDC-0917 binds to the Smac binding
groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP)
and the cellular IAPs 1 and 2. This inhibits the activities of these IAPs and promotes
the induction of apoptosis through apoptotic signaling pathways. IAPs are overexpressed
by many cancer cell types and suppress apoptosis by binding to and inhibiting active
caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains.;
UNII : KWH46ZDG32;
InChIKey : HSHPBORBOJIXSQ-HARLFGEKSA-N;
CAS number : 1446182-94-0;
Molecule name : GDC-0917; CUDC 427; RG-7459; RG 7459; CUDC-427;
NCI Metathesaurus CUI : CL433733;
Origin ID : C103825;
UMLS CUI : C3641627;
Semantic type(s)
- concept_is_in_subset
