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-172919
    PDEδ/NAMPT IN-1
    		Inhibitor
    PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD+), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.
    PDEδ/NAMPT IN-1
  • HY-175294
    PD-L1/Nampt-IN-1
    		Inhibitor
    PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma.
    PD-L1/Nampt-IN-1
  • HY-147838
    Nampt-IN-9
    		Inhibitor
    Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma research.
    Nampt-IN-9
  • HY-181350
    CAIX/XII/NAMPT-IN-1
    		Inhibitor
    CAIX/XII/NAMPT-IN-1 is a triple inhibitor of carbonic anhydrase IX/XII and nicotinamide phosphoribosyltransferase (NAMPT) with a hCA IX Ki of 78.1 nM, hCA XII Ki of 64.4 nM, and hNAMPT IC50 of 168 nM. CAIX/XII/NAMPT-IN-1 induces apoptosis, ROS accumulation, suppresses ERK/AKT signaling, inhibits DNA synthesis, and causes mitochondrial dysfunction. CAIX/XII/NAMPT-IN-1 exerts antiproliferative effects against multiple cancer cells under normoxic and hypoxic conditions. CAIX/XII/NAMPT-IN-1 can be used for the research of cancer, such as renal carcinoma, glioblastoma and colorectal cancer.
    CAIX/XII/NAMPT-IN-1
  • HY-W587952
    Gibberellin A34
    		Inhibitor
    Gibberellin A34 is a Hypoxanthine guanine phosphoribosyltransferase 1 (HPRT1) inhibitor that can be isolated from immature seeds of Calonyction aculeatum. Gibberellin A34 can be used for studies on plant growth and development regulation.
    Gibberellin A34
  • HY-163280
    JGB-1-155
    		Activator
    JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD+ in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells .
    JGB-1-155
  • HY-164759
    Nampt-IN-13
    		Inhibitor
    Nampt-IN-13 (example 58m) is a NAMPT inhibitor that can be used in the synthesis of Antibody-drug Conjugate (ADC).
    Nampt-IN-13
  • HY-163440
    PROTAC NAMPT Degrader-1
    		Degrader
    PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells. (Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker).
    PROTAC NAMPT Degrader-1
  • HY-162124
    HDAC/NAMPT-IN-1
    		Inhibitor
    HDAC/NAMPT-IN-1 (compound 39h) is a dual inhibitor of HDAC and NAMPT with IC50 values of 0.72-37081 nM and 1618 nM.
    HDAC/NAMPT-IN-1
  • HY-181880
    PROTAC NAMPT Degrader-28
    		Degrader
    PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research.
    PROTAC NAMPT Degrader-28
  • HY-181881
    MV78-OH
    		Ligand
    MV78-OH is a NAMPT ligand that can be used as a target protein ligand to synthesize NAMPT-targeting PROTACs, such as PROTAC NAMPT Degrader-28 (HY-181880).
    MV78-OH
  • HY-158319
    Mutant IDH1/NAMPT-IN-1
    		Inhibitor
    Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively.
    Mutant IDH1/NAMPT-IN-1
  • HY-176237
    Nampt-IN-16
    		Inhibitor
    Nampt-IN-16 (Compound 9a) is an orally active NAMPT inhibitor with an IC50 of 0.15 μM. Nampt-IN-16 can reduce intracellular NAD+ and ATP levels. Nampt-IN-16 can inhibit the proliferation, migration, and invasion, induce cell cycle arrest and apoptosis, and alter cellular metabolism of gastric cancer cells. Nampt-IN-16 can be used in the research of tumors such as gastric cancer.
    Nampt-IN-16
  • HY-163499
    NAMPT activator-7
    		Activator
    NAMPT activator-7 (Compound 232) is an activator for nicotinamide phosphoribosyltransferase (NAMPT), with EC50 < 0.5 μM. NAMPT activator-7 activates NAMPT in cells U2OS with cellular EC50 of < 0.5 μM.
    NAMPT activator-7
  • HY-148572
    NAMPT/IDO1-IN-1
    		Inhibitor
    NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel.
    NAMPT/IDO1-IN-1
  • HY-182062
    NAMPT activator-9
    		Activator
    NAMPT activator-9 (Compound DIPM) is an allosteric, non-competitive NAMPT activator, with an EC50 of 3.366 μM against hNAMPT. NAMPT activator-9 enhances the enzymatic activity of NAMPT via an allosteric, non-competitive mechanism. NAMPT activator-9 increases intracellular NAD+ levels. NAMPT activator-9 restores myotube diameter and reduces the expression of atrophy markers Atrogin-1 and MuRF1. NAMPT activator-9 is applicable to research related to muscle atrophy.
    NAMPT activator-9
  • HY-186105
    P7C3-S243
    P7C3-S243 is a brain-penetrant P7C3 class of neuroprotective agent. P7C3-S243 augments synthesis of nicotinamide adenine dinucleotide through activation of the metabolic enzyme nicotinamide phosphoribosyltransferase. P7C3-S243 shows potent neuroprotective efficacy in parkinson’s disease mice models. P7C3-S243 can be used for the research of parkinson’s disease.
    P7C3-S243
  • HY-181254
    PARP1/NAMPT-IN-1
    		Inhibitor
    PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC50 values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
    PARP1/NAMPT-IN-1
  • HY-159009
    MS7
    		Inhibitor
    MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). NAMPT is overexpressed in many cancer cells to meet the continuous replenishment of NAD+ required for rapid proliferation. MS7, as a NAMPT target protein ligand, can be used to synthesize PROTAC A7, which is an effective NAMPT degrader. MS7 can be used in cancer research.
    MS7
  • HY-147756
    Nampt-IN-7
    		Inhibitor
    Nampt-IN-7 (compound GF8) is a potent NAMPT inhibitor, with an IC50 of 7.31 μM. Nampt-IN-7 also displays cytotoxic activity against human HepG2 hepatocellular carcinoma cell line with an IC50 of 24.28 μM.
    Nampt-IN-7
Cat. No. Product Name / Synonyms Application Reactivity