1. Metabolic Enzyme/Protease
  2. 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 (45):

Cat. No. Product Name Effect Purity
  • HY-50876
    (E)-Daporinad Inhibitor 99.91%
    (E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.
  • HY-10079
    CHS-828 Inhibitor 99.74%
    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[1].
  • HY-144776
    NAT Activator 99.56%
    NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases[1].
  • HY-126255
    SBI-797812 Activator 99.74%
    SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+ in mice[1][2].
  • HY-15766
    GNE-617 Inhibitor 99.69%
    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-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[1].
  • HY-163445
    NAMPT activator-6 Activator
    NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation[1].
  • HY-162519
    LZFPN-90 Inhibitor
    LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system[1].
  • HY-161515
    BRD4/NAMPT-IN-1 Inhibitor
    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[1].
  • HY-15766A
    GNE-617 hydrochloride Inhibitor 99.28%
    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-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[1].
  • HY-12628
    GNE-618 Inhibitor 99.89%
    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[1].
  • HY-162269
    Nampt activator-5 Activator
    Nampt activator-5 (compound C8) is a potent nicotinamide phosphoribosyltransferase (NAMPT) activator with a KD value of 6.19 µM. Nampt activator-5 shows a cellular antisenescence effect. Nampt activator-5 promotes the production of NAD+ in the brain and reduces the expression of age-related markers and secretory phenotypes. Nampt activator-5 has the potential for the research of age-related diseases[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[1].
  • 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[1].
  • 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 [1].
  • 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. (Srtucture Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker)[1].
  • HY-12808
    STF-118804 Inhibitor
    STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.
  • 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[1].
  • 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[1].