CB30865

CB30865(ZM 242421) is a potent inhibitor of Nampt , an enzyme present in the NAD biosynthetic pathway. IC50 value:Target: NamptCancer cells develop dependence on Nampt due to increased energy requirements and the elevated activity of NAD consuming enzymes such as sirtuins and mono and poly(ADP-ribose) polymerases (PARPs). These findings suggest new chemical starting points for Nampt inhibitors and further implicate this enzyme as a target in cancer.

Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

Research Areas >> Cancer

[1]. Lockman JW, et al. Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as potent inhibitors of nicotinamide phosphoribosyltransferase (Nampt). J Med Chem. 2010 Dec 23;53(24):8734-8746.

[2]. Fleischer TC, et al. Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound. Chem Biol. 2010 Jun 25;17(6):659-664.

[3]. Bavetsias V, et al. The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. J Med Chem. 2002 Aug 15;45(17):3692-3702.

[4]. Skelton LA, et al. Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action. Cytometry. 1998 Sep 1;33(1):56-66.

FK866 (APO866, Daporinad) | P7C3 | STF 118804 | GMX1778 | KPT-9274 | GNE-617 | Nampt-IN-1 | CB 300919