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-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
  • HY-157421
    Nampt activator-4
    		Modulator
    Nampt activator-4 is a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of 0.058 μM. Nampt activator-4 can enhance the nicotinamide adenine dinucleotide (NAD+) in cells.
    Nampt activator-4
  • 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.
    NAMPT activator-6
  • HY-162537
    LYP-8
    		Inhibitor
    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-147193A
    Nampt-IN-10 trihydrochloride
    		Inhibitor
    Nampt-IN-10 trihydrochloride (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 trihydrochloride shows cellular potency to A2780 and CORL23 cell lines with IC50 values of 5 and 19 nM, respectively. Nampt-IN-10 trihydrochloride can be used as a novel non-antimitotic payload for antibody-drug conjugate (ADC).
    Nampt-IN-10 trihydrochloride
  • HY-147795
    Nampt-IN-8
    		Inhibitor
    Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS.
    Nampt-IN-8
  • HY-147656
    NAMPT degrader-1
    		Inhibitor
    NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency.
    NAMPT degrader-1
  • HY-155506
    NAMPT degrader-3
    		Degrader
    NAMPT degrader-3 (compound C5) is a NAMPT degrader, depending on VHL- and proteasome manner. NAMPT degrader-3 displays cytotoxicity and inhibits A2780 cells proliferation.
    NAMPT degrader-3
  • 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.
    LZFPN-90
  • HY-163500
    NAMPT activator-8
    		Activator
    NAMPT activator-8 (Compound 278) is an activator for nicotinamide phosphoribosyltransferase (NAMPT), with EC50 < 0.5 μM. NAMPT activator-8 activates NAMPT in cells U2OS with cellular EC50 of < 0.5 μM.
    NAMPT activator-8
  • HY-125147
    A-1293201
    		Inhibitor
    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-10079A
    CHS-828 (nicotinate)
    		Inhibitor
    CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity.
    CHS-828 (nicotinate)
  • HY-161180
    Antitumor agent-136
    		Inhibitor
    Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC50 of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition.
    Antitumor agent-136
Cat. No. Product Name / Synonyms Application Reactivity