nicotinamide phosphoribosyltransferase

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

Nampt-IN-5 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

The P7C3 class of neuroprotective aminopropyl carbazoles has been shown to block neuronal cell death in models of neurodegeneration. We now show that P7C3 molecules additionally preserve axonal integrity after injury, before neuronal cell death occurs, in

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM).

GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.

Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

STF-118804, a highly specific NAMPT inhibitor, reduces the viability of most B-ALL cell lines with an IC50 of less than 10 nM.

OT-82 is a potent, selective, and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

Nampt-IN-3 simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC (IC50s of 31 nM and 55 nM, respectively).

CB30865 (ZM 242421) is a selective and highly effective nicotinamide phosphoribosyltransferase (Nampt) inhibitor with potential antitumor activity.

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.

Namptactivator-5 (compound C8) is a potent activator of nicotinamide phosphoribosyltransferase (NAMPT), with a KD value of 6.19 µM. This compound demonstrates cellular anti-aging effects by promoting NAD+ production in the brain and reducing markers and secretory phenotypes associated with aging. Namptactivator-5 holds potential for researching age-related diseases.

NAMPTactivator-8 (Compound 278) is an activator of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of less than 0.5 μM. It activates NAMPT in U2OS cells with a cellular EC50 also below 0.5 μM.

Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutantIDH1) with an IC50 of 14.93 nM, and nicotinamide phosphoribosyltransferase (NAMPT) with an IC50 of 12.56 nM. This compound can induce apoptosis and effectively crosses the blood-brain barrier.

NAMPTactivator-7 (Compound 232) is an activator of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of less than 0.5 μM. It effectively stimulates NAMPT in U2OS cells, demonstrating a cellular EC50 of less than 0.5 μM.

SIAIS630121-NC serves as the negative control for the degradation product SIAIS630121 of NAMPT (nicotinamide phosphoribosyltransferase).

SIAIS630120-NC is the negative control for the degradation product of NAMPT (nicotinamide phosphoribosyltransferase), known as SIAIS630120.

PD-L1/Nampt-IN-1 is an orally active inhibitor that targets both PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase), with IC50 values of 63 nM and 582 nM, respectively. It exhibits cross-species affinity, with KD values of 52.6 nM for hPD-L1 and 49.1 nM for mPD-L1. This compound effectively suppresses tumor growth by activating the tumor immune microenvironment and is applicable in melanoma research.

GNE-617 hydrochloride is a potent and competitive inhibitor of nicotinamide phosphoribosyltransferase (IC50: 5nM). GNE-617 hydrochloride reduces the NAD levels in a > 95% reduction in both NAPRT1-deficient and NAPRT1-proficient cell lines and exerts (EC50

7-Bromoheptanoic acid is a building block.1,2It has been used in the synthesis of azide-based nicotinamide phosphoribosyltransferase (Nampt) inhibitors with anticancer activity and SAHA derivatives that inhibit histone deacetylases (HDACs). 1.Colombano, G., Travelli, C., Galli, U., et al.A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistryJ. Med. Chem.53(2)616-623(2010) 2.Suzuki, T., Nagano, Y., Kouketsu, A., et al.Novel inhibitors of human histone deacetylases: Design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamatesJ. Med. Chem.48(4)1019-1032(2005)

GPP 78 hydrochloride is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt) with an IC50 of 3 nM for NAD depletion. GPP 78 hydrochloride is toxic to neuroblastoma cells SH-SY5Y via induction of autophagy with an IC50 of 3.8 nM. GPP78 has anticancer and anti-inflammatory effects.

NAT is a nicotinamide phosphoribosyltransferase (NAMPT) activator that increases intracellular NAD levels and induces subsequent metabolic and transcriptional reprogramming. It exhibits neuroprotective effects in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model and may be employed in studies of neurodegenerative diseases or conditions associated with reduced NAD levels.