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

NAMPT

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.

NAMPT Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-50876
    (E)-Daporinad Inhibitor 99.94%
    (E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.
  • HY-126255
    SBI-797812 Inhibitor 98.20%
    SBI-797812 is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT with EC50 of 0.37 μM. SBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+. Dosing of mice with SBI-797812 elevates liver NAD+.
  • HY-10079
    CHS-828 Inhibitor 99.35%
    CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity.
  • HY-15766
    GNE-617 Inhibitor 99.85%
    GNE-617 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.
  • HY-136241
    OT-82 Inhibitor 99.84%
    OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD+ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies.
  • HY-10080
    Teglarinad chloride Inhibitor 98.07%
    Teglarinad chloride (GMX1777) is a prodrug 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.
  • HY-130606
    Nampt-IN-5 Inhibitor 99.21%
    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.
  • HY-12971
    Nampt-IN-1 Inhibitor 99.48%
    Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
  • HY-12808
    STF-118804 Inhibitor 98.55%
    STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.
  • HY-12628
    GNE-618 Inhibitor 98.14%
    GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.
  • HY-14373
    CB30865 Inhibitor 98.05%
    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).
  • 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.
  • HY-15766A
    GNE-617 hydrochloride Inhibitor 99.15%
    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.
  • HY-14375
    CB 300919 Inhibitor 98.53%
    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.
  • HY-112615
    NAMPT inhibitor-linker 1 Inhibitor
    NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
  • HY-101280
    LB-60-OF61 Inhibitor
    LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.
  • HY-108701
    Nampt-IN-3 Inhibitor
    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.
  • HY-112616
    NAMPT inhibitor-linker 2 Inhibitor
    NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
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