Home > Inhibitors & Agonists > Metabolic Enzyme/Protease > NAMPT
Cat. No. Product name CAS No.
DC6901 Daporinad(FK866,APO866) Featured

APO866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM.

DC8139 GMX1778(CHS-828) Featured

CHS-828 is a pyridyl cyanoguanidine anti-tumor agent that has been identified as a competitive inhibitor of Nampt as well as an inhibitor of NF-κB pathway activity.

DC10665 LSN3154567(Nampt-IN-1) Featured

LSN3154567 is a novel inhibitor of NAMPT with IC50 of 18 nM (NCI-H1155 cell), 49 nM (Calu-6 cell), 333 nM (HCC1937 cell), and 389 nM (MCF-7 cell), respectively.

DC7573 STF-118804 Featured

STF-118804 is a highly specific NAMPT inhibitor.

DC11492 GMX-1777 chloride

The water-soluble prodrug of GMX-1778 (CHS-828), which is a potent and specific inhibitor of the NAD(+) biosynthesis enzyme NAMPT with IC50 of <20 nM.

DC28672 Nampt-IN-5

Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.

DC28969 GPP78

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.

DC46694 OT-82 Featured

OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively.

DC70436 GNI-50

GNI-50 is a potent, selective Nampt inhibitor with enzyme IC50 of 7 nM, A2780 cellular IC50 of 32 nM.GNI-50 showed excellent in vivo antitumor efficacy when dosed orally in an A2780 ovarian tumor xenograft model (TGI of 97% was observed on day 17).

DC70637 NAMPT activator (NAT)

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.NAMPT activator (NAT) markedly increased the catalytic activity (Vmax) of NAMPT with higher Michaelis constants (Km) for both substrates, NAM, and PRPP.The stoichiometry analysis revealed that NAT bound to NAMPT at a 1:1 ratio, NAT may function as a reversible activator during the kinetic assay, and has no effect on NMNAT1 enzyme activity.

DC70638 NAMPT activator (NAT-5r)

NAMPT activator (NAT-5r) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 180 nM, 3-fold improved activity over NAT.NAMPT activator (NAT-5r) had no effect on NMNAT1 enzyme activity, both NAMPT mutants of K189R and K189A reduced the binding affinity of NAT-5r.NAMPT activator (NAT-5r) treatment significantly enhanced NAD content in NAMPT-WT cells, but not in NAMPT-CRISPR cells.Treatment of NAT-5r at 3 μM concentrations for 4 h induced significant elevation of cellular NAD.NAMPT activator (NAT-5r) induced subsequent metabolic and transcriptional reprogramming, promoted proliferation and maintain the self-renewal of NSCs and protects peripheral sensory neurons from paclitaxel-(PTX) induced damage in mouse model.

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