nampt activator-1

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.

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].

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 activator-4, a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT), has an EC50 of 0.058 μM and can enhance nicotinamide adenine dinucleotide (NAD+) levels in cells [1].

NAMPT activator-6, a regulatory molecule for the optical control system of NAMPT and NAD+, can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) for light-dependent, reversible regulation of NAMPT and NAD+, thereby reducing toxicity associated with inhibitor-based PS-PROTACs. This enables antitumor activity and in vivo modulation of NAMPT and NAD+ through optical manipulation [1].