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 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 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.

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

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

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

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].

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].

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

(E)-Daporinad (FK866) is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.

β-nicotinamide mononucleotide is a product of the nicotinamide-phosphate ribosyltransferase (NAMPT) reaction. β-nicotinamide mononucleotide's actions include its role in cellular biochemical function, cardioprotection, diabetes, obesity-related complications, and Alzheimer's disease.

OT-82 is a potent, selective and orally active NAMPT inhibitor.

LB-60-OF61 is a NAMPT inhibitor, a NAMPT inhibitor that displays antiproliferative activity against MYC oncogene-dependent cancer cell lines.

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)

GNE-617 hydrochloride is a specific inhibitor of NAMPT and inhibits NAMPT activity (IC50: 5 nM).

NAMPT inhibitor

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

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

STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.

CB30865 is a potent inhibitor of Nampt, an enzyme present in the NAD biosynthetic pathway.

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

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].

A-1293201 is a potent and selective NAMPT inhibitor.

Teglarinad chloride (GMX-1777 chloride) is a potent inhibitor of NAMPT, the precursor of GMX1778.Teglarinad chloride has antitumor activity and acts by interfering with DNA repair and inhibiting angiogenesis.

Antitumor Agent-136 (Compound 17), a broad-spectrum antitumor agent and NAMPT inhibitor, exhibits potent activity with an IC50 of 9.5 nM. It efficiently lowers intracellular and extracellular NAMPT protein levels via the ubiquitin proteasome pathway, achieving effective tumor inhibition [1].

GPP 78 hydrochloride is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt) with an IC50 of 3 nM for NAD depletion. GPP 78 hydrochloride is toxic to neuroblastoma cells SH-SY5Y via induction of autophagy with an IC50 of 3.8 nM. GPP78 has anticancer and anti-inflammatory effects.

LB-60-OF61 hydrochloride is a highly effective inhibitor of NAMPT, a key enzyme involved in the transfer of nicotinamide phosphoribosyl groups. This compound, known for its cytotoxic properties, specifically targets cell lines that overexpress MYC, thereby demonstrating selectivity in its action.

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

CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, doxorubicin in 47%, etoposide in 38% and Ara-C in 14% of AML samples.

GPP78 is a potent inhibitor of Nampt (IC50: 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion). GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells (IC50: 3.8 nM by inducing autophagy). GPP78 has anti-cancer and anti-inflammatory effect

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