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-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.

(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.

LB-60-OF61 is a NAMPT inhibitor that exhibits antiproliferative activity against MYC oncogene-dependent cancer cell lines (brackets).

OT-82 is a potent, selective, and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 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.

GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of 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].

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.

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.