nampt

Nampt activator-2 is a NAMPT activator (EC50: 0.023 μM). Nampt activator-2 has an affinity for CYP2C9, 2D6, and 2C19 with affinity values of 0.060 μM, 0.41 μM, and 0.59 μM, respectively.Nampt activator-2 can be used in the study of atherosclerosis, obesity, type II diabetes, insulin resistance, and type I diabetes.

Nampt-IN-5 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

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.

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

Nampt-IN-13 (example 58m) is an NAMPT inhibitor used in the synthesis of antibody-drug conjugates (ADCs).

Nampt-IN-15 (Example 3) is a Nampt inhibitor that exhibits cytotoxic effects on various cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13. The respective IC50 values for these cell lines are 38.5 nM, 8 nM, 8.5 nM, and 7 nM.

Nampt-IN-14 (example 3) is an effective NAMPT inhibitor with an IC50 of 0.2 nM, suited for use in the synthesis of antibody-drug conjugates (ADCs).

Daporinad hydrochloride (FK 866 hydrochloride) is a potent nicotinamide-phosphate ribosyltransferase (NAMPT) inhibitor with potential anti-tumor and anti-angiogenic activity that induces apoptosis in tumor cells.Daporinad hydrochloride can be used in the study of inflammation and cancer.

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

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

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 inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

PARP NAMPT-IN-1 (Compound 13j) is a dual-target inhibitor of PARP and NAMPT, with IC50 values of 0.8 nM for PARP1 and 18 nM for NAMPT. It suppresses breast cancer cell proliferation and migration, inducing apoptosis. PARP NAMPT-IN-1 is applicable for research on triple-negative breast cancer.

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].

Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer properties that can be used to study ductal adenocarcinoma of the pancreas.

Nampt-IN-8 is a NAMPT inhibitor (IC50: 0.183 μM) and a good substrate for NQO1. Nampt-IN-8 induces reactive oxygen species (ROS) production and apoptosis.

Nampt-IN-10 TFA (compound 4) is a phosphoribosyltransferase (NAMPT) inhibitor with cellular efficacy against A2780 (IC50: 5 nM) and CORL23 (IC50: 19 nM), and can be used as a non-antimitotic payload for ADCs.

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-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].

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 degrader-2, a fluorescent PROTAC, exhibits efficient degradation of NAMPT at an IC50 of 41.9 nM. It operates by binding to both NAMPT and VHL, initiating the formation of a ternary complex that triggers NAMPT degradation through the ubiquitin-proteasome system (UPS). This activity significantly lowers NAD+ levels and displays potent antitumor effects [1].

HDAC NAMPT-IN-1 (compound 39h) simultaneously inhibits HDAC and NAMPT, exhibiting IC 50 values ranging from 0.72 to 37081 nM for HDAC and 1618 nM for NAMPT [1].