NCIt definition : An orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential
antineoplastic activity. Upon administration, GS/pan-Notch inhibitor AL102 binds to
GS and blocks 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 of
tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway
plays an important role in tumor cell proliferation and survival. The integral membrane
protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane
proteins, such as Notch receptors, at residues within their transmembrane domains
and leads to their activation.;
UNII : LSK1L593UU;
CAS number : 1584647-27-7; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1584647-27-7
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G-SRS /a ;
Molecule name : BMS-986115; AL 102; AL-102; WHG 626; WHG-626;
Semantic type(s)