Preferred Label : Gamma-Secretase Inhibitor LY3039478;
Obsolete resource : true;
NCIt synonyms : 4,4,4-Trifluoro-N-((S)-1-(((S)-5-(2-hydroxyethyl)-6-oxo-6,7-dihydro-5H-benzo[d]pyrido[2,3-b]azepin-7-yl)amino)-1-oxopropan-2-yl)butanamide;
NCIt definition : An orally available inhibitor of the integral membrane protein gamma-secretase (GS),
with potential antineoplastic activity. Upon administration, gamma-secretase inhibitor
LY3039478 binds to the GS protease complex, thereby blocking the proteolytic cleavage
and release of the Notch intracellular domain (NICD), which would normally follow
ligand binding to the extracellular domain of the Notch receptor. This prevents both
the subsequent translocation of NICD to the nucleus to form a transcription factor
complex and the expression of Notch-regulated genes. This results in the induction
of apoptosis and the inhibition of growth in tumor cells that overexpress Notch. Overexpression
of the Notch signaling pathway plays an important role in tumor cell proliferation
and survival.;
NCIt note : See 'Crenigacestat(C171871)';
Concept status : Retired_Concept;
CAS number : 1421438-81-4; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1421438-81-4
alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo
G-SRS /a ;
Molecule name : JSMD194; LY-3039478; LY 3039478;
NCI Metathesaurus CUI : CL446654;
Origin ID : C121535;
UMLS CUI : C4053622;
Semantic type(s)
- has_target
