nampt-in-1

Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

NAMPT Activator-1 (compound 1) is an effective and specific activator of niacinamide phosphotransferase (Compound 1) with a wide range of EC50 (3.3-3.7 μM). NAMPT activator-1 effectively protects cultured cells from FK866-mediated toxicity and is a potential neuroprotective compound.

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

NAMPT Degrader-1 (Compound A3), a nicotinamide phosphoribosyltransferase (NAMPT) degrader, exhibits potent antitumor activity in cells by specifically inducing the degradation of NAMPT via the autophagy-lysosomal pathway, with an inhibitory concentration (IC50) of 0.023 μM [1].

Nampt-IN-10 trihydrochloride (Compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor exhibiting cellular potency against A2780 and CORL23 cell lines, with IC50 values of 5 nM and 19 nM, respectively. It holds potential as a novel non-antimitotic payload for antibody-drug conjugate (ADC) [1].

7-Bromoheptanoic acid is a building block.1,2It has been used in the synthesis of azide-based nicotinamide phosphoribosyltransferase (Nampt) inhibitors with anticancer activity and SAHA derivatives that inhibit histone deacetylases (HDACs). 1.Colombano, G., Travelli, C., Galli, U., et al.A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistryJ. Med. Chem.53(2)616-623(2010) 2.Suzuki, T., Nagano, Y., Kouketsu, A., et al.Novel inhibitors of human histone deacetylases: Design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamatesJ. Med. Chem.48(4)1019-1032(2005)

NAMPT Activator-3, a derivative of NAT, is a potent activator of NAMPT, demonstrating an EC50 of 2.6 μM and KD of 132 nM. It effectively shields cultured cells against toxicity induced by FK866 and has demonstrated significant neuroprotective effects in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model, without any apparent toxicity [1].

Nampt-IN-7, also known as compound GF8, is a powerful NAMPT inhibitor exhibiting an IC50 value of 7.31 μM. It possesses significant cytotoxic effects against the human HepG2 hepatocellular carcinoma cell line, with an IC50 value of 24.28 μM [1].

NAT, an initial NAMPT activator, targets NAMPT, a crucial enzyme in the NAD salvage pathway and a key focal point for researching a variety of diseases linked to NAD depletion, including neurodegenerative diseases[1].

KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.