Nampt-IN-3 simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC (IC50s of 31 nM and 55 nM, respectively).

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 Degrader-3 (compound C5) is a NAMPT degrader that functions through a VHL- and proteasome-dependent mechanism. It exhibits cytotoxic properties and inhibits the proliferation of A2780 cells [1].

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.