2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. NAMPT

NAMPT

Nicotinamide phosphoribosyl transferase; PBEF; Visfatin; pre-B cell-enhancing factor; Pre-B cell colony enhancing factor

NAMPT

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Nicotinamide phosphoribosyltransferase (NAMPT) is the rate-limiting enzyme which catalyzes the conversion of nicotinamide (NAM) and phosphoribosyl-pyrophosphates to nicotinamide mononucleotide (NMN) in the mammalian nicotinamide adenine dinucleotide (NAD+) synthetic salvage pathway. NAMPT exists in two forms, intracellular NAMPT (iNAMPT) and extracellular NAMPT (eNAMPT).

iNAMPT levels are high in brown adipose tissue (BAT), liver and kidney, intermediate in white adipose tissue (WAT), lung, spleen, testes and skeletal muscle, and undetectable in brain and pancreas. eNAMPT, thought to be produced through post-translational modification of iNAMPT, is released into plasma predominantly from adipose tissue, where it catalyses the synthesis of NMN. Although intracellular NAMPT is a key enzyme in controlling NAD metabolism, eNAMPT has been reported to function as a cytokine, with many roles in physiology and pathology. Circulating eNAMPT has been associated with several metabolic and inflammatory disorders, including cancer.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161515
    BRD4/NAMPT-IN-1
    		Inhibitor 99.45%
    BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects.
    BRD4/NAMPT-IN-1
  • HY-148815
    Nampt activator-1
    		Activator 98.63%
    Nampt activator-1 is a nicotinamide phosphoribosyltransferase (NAMPT) activator, with an EC50 of 3.3~3.7 μM. Nampt activator-1 enhances the enzymatic activity of NAMPT. Nampt activator-1 can be used for research related to metabolic disorders.
    Nampt activator-1
  • HY-P2940
    NADase
    NADase is an ectoenzyme/membrane-bound enzyme targeting nicotinamide adenine dinucleotide (NAD+). NADase regulates intracellular NAD+ homeostasis by hydrolyzing NAD+ into nicotinamide mononucleotide (NMN) and ADP-ribose. NADase is promising for research of autoimmune diseases (e.g., systemic sclerosis, systemic lupus erythematosus) and aging-related disorders.
    NADase
  • HY-14373
    CB30865
    		Inhibitor 98.75%
    CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC50 values in the 1-10 nM range). CB30865 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CB30865
  • HY-148822
    Nampt activator-2
    		Activator 98.79%
    Nampt activator-2 (compound 34) is a potent NAMPT activator, with EC50 of 0.023 μM. Nampt activator-2 shows moderate activity against CYP2C9 (0.060 μM), 2D6 (0.41 μM) and 2C19 (0.59 μM).
    Nampt activator-2
  • HY-10080
    Teglarinad chloride
    		Inhibitor 99.67%
    Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.
    Teglarinad chloride
  • HY-108701
    Nampt-IN-3
    		Inhibitor 98.97%
    Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
    Nampt-IN-3
  • HY-N3225
    Myricanol
    		Activator 98.93%
    Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation.
    Myricanol
  • HY-157421
    Nampt activator-4
    		Activator 98.87%
    Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD+, thereby enhancing enzymatic activity and significantly increasing intracellular NAD+ levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders.
    Nampt activator-4
  • HY-15766A
    GNE-617 hydrochloride
    		Inhibitor 99.16%
    GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
    GNE-617 hydrochloride
  • HY-162537
    LYP-8
    		Inhibitor 99.89%
    LYP-8 is a potent and effective NAMPT degrader with maximum degradation of 97% at 0.5 μM in SKOV-3 cells. LYP-8 shows anti-cancer activity in vivo and in vitro(Sturcture Note:(Blue: Cereblon ligand (HY-112078), Black: linker (HY-128801)；Pink: Nampt inhibitor Nampt-IN-11 (HY-158689)).
    LYP-8
  • HY-130606
    Nampt-IN-5
    		Inhibitor 98.02%
    Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
    Nampt-IN-5
  • HY-14374
    GPP78
    		Inhibitor 99.0%
    GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
    GPP78
  • HY-101280
    LB-60-OF61
    		Inhibitor 99.25%
    LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.
    LB-60-OF61
  • HY-14375
    CB 300919
    		Inhibitor 99.10%
    CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft. CB 300919 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CB 300919
  • HY-125147
    A-1293201
    		Inhibitor 99.82%
    A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD+/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079).
    A-1293201
  • HY-101280A
    LB-60-OF61 hydrochloride
    		Inhibitor
    LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.
    LB-60-OF61 hydrochloride
  • HY-161051
    Anticancer agent 177
    		Inhibitor
    Anticancer agent 177 (Compound 11b) is a NAMPT inhibitor and DNA alkylating agent. Anticancer agent 177 has antitumor activity in vitro and in vivo.
    Anticancer agent 177
  • HY-110319
    (E/Z)-Daporinad hydrochloride
    		Inhibitor
    (E/Z)-Daporinad hydrochloride ((E/Z)-FK866 hydrochloride) is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). (E/Z)-Daporinad hydrochloride induces apoptosis by specifically inhibiting NAMPT to gradually deplete intracellular NAD+. (E/Z)-Daporinad hydrochloride can be used in the study of cancer biology and inflammatory diseases.
    (E/Z)-Daporinad hydrochloride
  • HY-162269
    Nampt activator-5
    		Activator
    Nampt activator-5 is a NAMPT activator with a KD value of 6.19 μM. Nampt activator-5 activates the rate-limiting enzyme in NAD+ biosynthesis and promotes NAD+ production. Nampt activator-5 delays the senescence process of senescent hepatocytes, extends the lifespan of *Caenorhabditis elegans*, and alleviates age-related dysfunction and abnormal biomarkers in naturally aged mice. Nampt activator-5 can be used in aging research.
    Nampt activator-5
Cat. No. Product Name / Synonyms Application Reactivity