YO-01027 (Dibenzazepine; YO 01027)

Description: YO-01027 (also called dibenzazepine; DBZ; YO01027) is a novel, potent, orally bioavailable, dipeptidic inhibitor of the gamma-secretase with potential antineoplastic activity. It inhibits gamma-secretase with IC50s of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively. It shows high in vivo antitumor efficacy in C57BL/6 mice bearing MCF-7 tumors.

References: Mol Pharmacol. 2010; 77(4):567-74; Cancer Res. 2010; 70(2):709-18; Nature. 2005; 435(7044):959-63.

Chemical Name: (S)-2-(2-(3, 5-difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6, 7-dihydro-5H-dibenzo[b, d]azepin-7-yl)propanamide

SMILES Code: C[CH](NC(CC1=CC(F)=CC(F)=C1)=O)C(N[CH]2C(N(C)C3=CC=CC=C3C4=CC=CC=C24)=O)=O