RGNCY-0083 (35 Dual HDAC NAMPT inhibitor)

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Compound 35 is a novel potent dual NAMPT (nicotinamide phosphoribosyltransferase) and HDAC (histone deacetylase) inhibitor.  Compound 35 effectively induces cell death via the induction of apoptosis and autophagy.  It has significant anti-tumor efficacy in the HCT116 (human cancer cell line) xenograft model.  This compound provides an efficient multi-target strategy for the inhibition of cancer metabolism and epigenetics in tumor treatment. NAMPT IC50 = 31nM, HDAC1 IC50 = 55nM.

Systematic Name: N-(2-aminophenyl)-4-((5-(4-((pyridin-3-ylmethyl)carbamoyl)phenyl)-3H-1,2,4-triazol-3-yl)methyl)benzamide

Formula: C29H25N7O2
Mol Wt:  503.21

PMID: 28885834

Tags: NAMPT, Cancer, Apoptosis, autophagy, HDAC, RGNCY-0083, 35, epigenetic