RGNCY-0060 (MS0 NAMPT inhibitor)

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NAMPT (nicotinamide phosphoribosyltransferase)  is a promising therapeutic target for cancer.  MS0 is a novel NAMPT inhibitor with excellent in vitro activity (IC50 = 9.87 + 1.15 nM) and anti-proliferative activity against multiple human cancer cell lines (HepG2, A549, ad HCT116) and stem-like cancer cells.  MS0 specifically binds to the NAMPT target in living cells.  MS0 is a useful tool in developing NAMPT inhibitors as anti-cancer therapeutic agents.

Systematic Name:  N-(4-(piperidin-1-ylsulfonyl)phenyl)-N'-(pyridin-3-ylmethyl)ethene-1,1-diamine

SMILES:  C=C(NC1=CC=C(S(N2CCCCC2)(=O)=O)C=C1)NCC3=CN=CC=C3

Formula:  C19H24N4O2S

Mol Wt: 372.49

PMID:  26040985