Catalog No.
Product Name
Application
Product Information
Citations
-
NAMPT inhibitor
CHS-828 is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM. -
NAMPT activator
P7C3-A20 is a potent neuroprotective agent.- Oku H, .et al. , Invest Ophthalmol Vis Sci, 2017, Sep 1;58(11):4877-4888 PMID: 28973334
- Oku H, .et al. , Jpn J Ophthalmol, 2017, Mar;61(2):195-203 PMID: 28032230
-
NAMPT activator
(R)-P7C3-Ome is a methoxy derivative of parent compound P7C3, an aminopropyl carbazole that exhibits antidepressant and neuroprotective activities. -
NAMPT inhibitor
STF 118804 is a highly specific NAMPT inhibitor that reduces the viability of most B-ALL cell lines with high potency IC50 values in the low nanomolar range and improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia. -
PAK4/NAMPT Inhibitor
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. -
NAMPT activator
SBI-797812 is a novel NAMPT activator, elevating liver NAD+, turning NAMPT into a "super catalyst" that more efficiently generates NMN. -
NAMPT 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. -
NAMPT inhibitor
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines. -
NAMPT inhibitor
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM. -
BRD4/NAMPT inhibitor
BRD4/NAMPT-IN-1 (Compound A2) is a dual inhibitor of NAMPT and BRD4, with IC₅₀ values of 35 nM and 58 nM, respectively. It suppresses the growth and migration of hepatocellular carcinoma cells and induces apoptosis. In the HCCLM3 xenograft mouse model, BRD4/NAMPT-IN-1 exhibits potent anticancer activity without apparent toxicity. -
PROTAC Nampt Degrader
Nampt degrader-2 is a potent PROTAC designed to target and degrade nicotinamide adenine dinucleotide (NAD+) precursor NAMPT with an IC50 of 41.9 nM. By forming a ternary complex with NAMPT and VHL, it effectively induces degradation through the ubiquitin-proteasome system. This compound significantly reduces NAD+ levels and demonstrates remarkable antitumor activity, making it a valuable tool for cancer research and therapeutic exploration. -
Nampt Inhibitor
OT-82 is a selective, orally active inhibitor of Nicotinamide Adenine Dinucleotide Phosphate (NAMPT). It exhibits potent cytotoxicity specifically towards hematopoietic cells and induces cell death in a NAD+ dependent manner. Due to these properties, OT-82 shows potential as an innovative antineoplastic agent for investigating hematological malignancies. -
HDAC/NAMPT Inhibitor
HDAC/NAMPT-IN-1 is a potent dual inhibitor of histone deacetylases (HDAC) and nicotinamide adenine dinucleotide (NAD+) biosynthesis enzyme NAMPT, exhibiting IC50 values ranging from 0.72 to 37081 nM for HDAC and 1618 nM for NAMPT. This compound demonstrates significant potential in modulating cellular acetylation levels and metabolic processes associated with cancer and neurodegenerative diseases. Its application in research can facilitate studies on epigenetic regulation and NAD+ metabolism, contributing to a deeper understanding of cellular mechanisms and therapeutic strategies. -
NAMPT Inhibitor
(E/Z)-Daporinad hydrochloride is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). By specifically targeting NAMPT, this compound induces apoptosis through the gradual depletion of intracellular NAD+. (E/Z)-Daporinad hydrochloride is utilized in research to explore mechanisms in cancer biology and inflammatory diseases. -
PDE6/NAMPT Inhibitor
PDEδ/NAMPT IN-1 is a potent dual inhibitor targeting phosphodiesterase 6 (PDE6) with a binding affinity of 0.410 nM and nicotinamide phosphoribosyl transferase (NAMPT) with an IC50 of 2.21 nM. This compound effectively disrupts KRAS-related signaling pathways and hampers the synthesis of nicotinamide adenine dinucleotide (NAD+), leading to apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 holds significant potential for advancing research in KRAS mutant pancreatic cancer. -
Nampt/SIRT1/PRDX5 Activator
Myricanol is a diarylheptanoid that acts as a Nampt activator, enhancing SIRT1 and PRDX5 activities. This compound exhibits notable anti-inflammatory properties and mitigates glucocorticoid-induced muscle atrophy while regulating inflammatory mediators. Additionally, it demonstrates growth inhibition and promotes apoptosis in human lung adenocarcinoma A549 cells. Myricanol is also implicated in neuroprotection via autophagy-mediated clearance of microtubule-associated protein tau and contributes to cardiovascular health by inhibiting key signaling pathways such as PDGFRβ and NF-κB. Its activation of mitochondrial transcription factor A (TFAM) further supports anti-renal fibrosis effects and improves insulin sensitivity through AMPK activation. -
Nampt Inhibitor
Daporinad hydrochloride is a potent non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki of 0.3 nM. It induces cellular effects such as depletion of NAD+ and ATP levels, suppression of the mTORC1 and MAPK/ERK signaling pathways, and activation of TFEB, leading to enhanced autophagy. Additionally, Daporinad hydrochloride disrupts the endoplasmic reticulum calcium pool, impairing T cell activation through diminished mitogen-induced calcium signaling. This compound is valuable for research in myeloma, liver cancer, and immunosuppression, with effects including cell cycle arrest and apoptosis in various cancer cell lines. -
NAMPT Inhibitor
Nampt-IN-8 is a selective inhibitor of Nicotinamide Adenine Dinucleotide Phosphate (NAMPT) with an IC50 value of 0.183 μM. This compound effectively induces apoptosis in cultured cells and enhances reactive oxygen species (ROS) production. It is a valuable tool for research on metabolic regulation and cellular stress responses, particularly in studies related to cancer and neurodegenerative diseases. -
PARP/NAMPT Inhibitor
PARP1/NAMPT-IN-2 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 0.8 nM and 18 nM, respectively. This compound effectively inhibits cell proliferation and migration, while inducing apoptosis in breast cancer cells. PARP1/NAMPT-IN-2 is particularly relevant for investigating therapeutic strategies in triple-negative breast cancer research. -
NAMPT Inhibitor
CHS-828 (nicotinate) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting an IC50 of less than 25 nM. This compound effectively reduces cellular levels of NAD+, leading to cytotoxic effects on cancer cells. CHS-828 is primarily utilized in cancer research applications, studying its anti-tumor properties and mechanisms of action in various malignancies. -
Mutant IDH1/NAMPT Inhibitor
Mutant IDH1/NAMPT-IN-1 is a dual inhibitor targeting mutant isocitrate dehydrogenase 1 (mutant IDH1) and nicotinamide phosphoribosyltransferase (NAMPT), with IC50 values of 14.93 nM and 12.56 nM, respectively. This compound effectively induces apoptosis, making it a valuable tool for research into cancer mechanisms and treatment strategies. Additionally, Mutant IDH1/NAMPT-IN-1 demonstrates the capability to cross the blood-brain barrier, enhancing its potential for applications in neurological studies and therapies. -
NAMPT Inhibitor
Nampt-IN-16 is a potent NAMPT inhibitor exhibiting an IC50 value of 0.15 μM. This compound effectively reduces intracellular levels of NAD+ and ATP, leading to the inhibition of proliferation, migration, and invasion in gastric cancer cells. Additionally, Nampt-IN-16 induces cell cycle arrest and apoptosis while altering cellular metabolism. It is a valuable tool for research focused on tumors, particularly gastric cancer. -
PARP1/NAMPT Inhibitor
PARP1/NAMPT-IN-1 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 1.2 nM and 6.7 nM, respectively. This compound disrupts the homologous recombination repair pathway, leading to the accumulation of DNA double-strand breaks, which induces cell cycle arrest and apoptosis. Additionally, PARP1/NAMPT-IN-1 demonstrates antimigratory effects and has shown significant antitumor activity in a breast cancer xenograft model. It is a valuable tool for research on triple-negative breast cancer (TNBC). -
PD-L1/NAMPT Inhibitor
PD-L1/Nampt-IN-1 is a dual inhibitor targeting PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50 values of 63 nM and 582 nM, respectively. This compound exhibits cross-species affinity with comparable KD values for human PD-L1 (52.6 nM) and mouse PD-L1 (49.1 nM). PD-L1/Nampt-IN-1 facilitates tumor growth inhibition by enhancing the tumor immune microenvironment, making it a valuable tool for research in melanoma studies. -
Nampt Inhibitor
GPP78 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis via the enzyme Nampt, demonstrating an IC50 of 3.0 nM. It exhibits cytotoxicity in the neuroblastoma SH-SY5Y cell line, with an IC50 of 3.8 nM, primarily by inducing autophagy. GPP78 serves as a valuable tool in cancer and inflammatory research, highlighting its potential therapeutic applications in oncology. -
NAMPT Degrader
NAMPT degrader-1 is an autophagosome-tethering compound (ATTEC) that targets nicotinamide phosphoribosyltransferase (NAMPT) with an IC50 of 0.023 μM. This compound effectively induces the degradation of NAMPT via the autophagy-lysosomal pathway, demonstrating significant antitumor activity in cellular models. NAMPT degrader-1 is valuable for research focused on cancer biology and the regulation of metabolic pathways involving NAD+ synthesis. -
Nampt Inhibitor
Nampt-IN-10 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting nanomolar inhibitory activity in various cancer cell lines, including MDA-MB453, NCI-N87, and NCI-H526. This compound can be utilized as a payload in antibody-drug conjugates (ADCs), where it has been shown to enhance anti-tumor efficacy. It serves as a valuable tool for researchers investigating NAMPT's role in cancer metabolism and therapeutic resistance. -
NAMPT Activator
Carba1 is a bifunctional carbazole derivative that acts as an activator of nicotinamide phosphoribosyltransferase (NAMPT), thereby enhancing NAD biosynthesis. This compound also binds to the colchicine site of tubulin, which can potentiate the anticancer effects of various chemotherapeutic agents, including Paclitaxel. Additionally, Carba1 displays neuroprotective properties and is capable of modulating cellular energy metabolism. It is suitable for research applications focused on cancer therapies and chemotherapy-induced peripheral neuropathy (CIPN). -
NAMPT Activator
NAMPT activator-9 is an allosteric, non-competitive activator of nicotinamide adenine dinucleotide (NAD+) biosynthesis, targeting the enzyme NAMPT with an EC50 of 3.366 μM. This compound enhances NAMPT's enzymatic activity, leading to increased intracellular NAD+ levels. Furthermore, NAMPT activator-9 has been shown to restore myotube diameter and decrease the expression of muscle atrophy markers Atrogin-1 and MuRF1, making it a valuable tool for research on muscle atrophy and related metabolic disorders. -
Nampt Inhibitor
Nampt-IN-5 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), a crucial enzyme in the NAD+ biosynthesis pathway. It demonstrates significant biological activity with cellular IC50 values of 0.7 nM against A2780 cells and 3.9 nM against COR-L23 cells, indicating strong efficacy in targeting cancer metabolism. In addition, Nampt-IN-5 inhibits CYP3A4 activity, making it relevant for studies on drug metabolism and potential interactions. Research applications include cancer cell metabolism and the investigation of therapeutic strategies targeting NAD+ pathways. -
NAMPT/IDO1 Inhibitor
NAMPT/IDO1-IN-1 is a dual inhibitor of NAMPT and IDO1, exhibiting IC50 values of 57.7 nM and 233 nM, respectively. By inhibiting NAMPT, this compound interferes with NAD+ biosynthesis, thereby suppressing the proliferation and migration of drug-resistant NSCLC cell lines, such as A549/R. Additionally, NAMPT/IDO1-IN-1 demonstrates significant antitumor activity in vivo and enhances the sensitivity of these resistant cells to paclitaxel treatment. This compound is valuable for research in cancer biology and the development of therapeutic strategies aimed at overcoming drug resistance. -
NAMPT Activator
NAT is a potent NAMPT activator, exhibiting an EC50 of 5.7 μM and a KD of 379 nM. As the rate-limiting enzyme in the NAD salvage pathway, NAMPT is crucial for maintaining cellular NAD levels, making it a valuable target for studying diseases linked to NAD depletion, such as neurodegenerative disorders. This compound is essential for research aiming to explore therapeutic strategies that enhance NAD metabolism and combat related pathologies. -
NAMPT Activator
Nampt Activator-3 is a potent NAD+ biosynthesis enhancer targeting nicotinamide phosphoribosyltransferase (NAMPT). With an EC50 of 2.6 μM and a KD of 132 nM, it effectively protects cultured cells from FK866-mediated toxicity. Additionally, Nampt Activator-3 demonstrates substantial neuroprotective effects in a mouse model of chemotherapy-induced peripheral neuropathy (CIPN), indicating its potential applicability in neuroprotection research and therapeutic interventions. -
NAMPT Inhibitor
Nampt-IN-10 TFA is a potent inhibitor of Nicotinamide Phosphoribosyltransferase (NAMPT). It exhibits significant cellular potency against A2780 and CORL23 cell lines, with IC50 values of 5 nM and 19 nM, respectively. This compound serves as a promising non-antimitotic payload for antibody-drug conjugates (ADCs) in cancer research, highlighting its potential in therapeutic applications targeting NAMPT-related metabolic pathways. -
Nampt Inhibitor
Nampt-IN-15 is an inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis through the inhibition of nicotinamide phosphoribosyltransferase (Nampt). It exhibits potent cytotoxicity in various cancer cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13, with IC50 values of 38.5 nM, 8 nM, 8.5 nM, and 7 nM, respectively. This compound is valuable for research applications focused on cancer metabolism and therapeutic strategies targeting NAMPT in tumor cells. -
NAMPT Activator
Nampt activator-1 is a potent activator of Nicotinamide phosphoribosyltransferase (NAMPT), exhibiting an EC50 in the range of 3.3 to 3.7 μM. This compound enhances NAMPT activity, which plays a crucial role in NAD+ biosynthesis. It has potential applications in research focused on metabolic disorders, neuroprotection, and aging-related studies, making it a valuable tool for investigating NAD+ metabolism and its implications in cellular energetics. -
NAMPT Inhibitor
GNE-618 is a potent inhibitor of nicotinamide phosphoribosyl transferase (NAMPT) with an IC50 of 6 nM. By depleting cellular NAD levels, GNE-618 induces apoptosis in tumor cells, exhibiting significant anti-tumor activity. This compound is primarily applied in cancer research, facilitating the study of NAD metabolism and its implications in oncology. -
NAMPT Activator
Nampt activator-2 is a potent NAMPT activator, demonstrating an EC50 value of 0.023 μM. This compound also exhibits moderate inhibitory activity against cytochrome P450 enzymes CYP2C9 (0.060 μM), CYP2D6 (0.41 μM), and CYP2C19 (0.59 μM). Its primary application lies in enhancing NAMPT-mediated pathways, making it a valuable tool for research in metabolic regulation and potential therapeutic interventions. -
NAMPT Activator
Nampt activator-4 is a potent activator of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting an EC50 of 0.058 μM in human cells and a binding affinity (Ka) of 0.08538 μM. By binding to the rear channel of NAMPT, it enhances enzyme activity and counteracts feedback inhibition caused by nicotinamide and NAD+, leading to increased cellular levels of nicotinamide adenine dinucleotide (NAD+). Nampt activator-4 can effectively shift the concentration-response curve of NAMPT inhibitors, making it a valuable tool for research into type 2 diabetes and metabolic regulation. Its stability in liver microsomes and impact on cytochrome P450 activity (CYP2D6 and CYP3A4) further support its potential utility in pharmacological studies. -
NAMPT Inhibitor
GNE-617 hydrochloride is a potent inhibitor of NAMPT (Nicotinamide adenine dinucleotide biosynthesis regulator) with an IC50 of 5 nM. This compound effectively disrupts NAMPT enzymatic activity, leading to decreased levels of NAD+ in cellular systems. GNE-617 has demonstrated significant efficacy in various xenograft cancer models, making it a valuable tool for investigating cancer metabolism and the therapeutic potential of targeting NAD+ synthesis. -
NAMPT Degrader
LYP-8 is a highly potent NAMPT degrader that achieves up to 97% degradation of NAMPT at a concentration of 0.5 μM in SKOV-3 cells. Its mechanism of action involves selective targeting for degradation, leading to significant anti-cancer effects both in vitro and in vivo. This compound is valuable for research applications focused on the modulation of NAD+ metabolism and the exploration of therapeutic strategies in cancer treatment. -
NAMPT Inhibitor
A-1293201 is a potent NAMPT inhibitor that demonstrates antitumor activity by reducing total cellular NAD+/NADH levels. This reduction leads to significant ATP depletion, ultimately resulting in the induction of cancer cell death. Additionally, A-1293201 effectively addresses the acquired resistance mechanism associated with the NAMPT Y18 mutant, providing a promising avenue for research in cancer treatment. -
NAMPT Inhibitor
LB-60-OF61 hydrochloride is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), demonstrating significant cytotoxic effects. This compound shows selective activity against MYC-overexpressing cell lines, making it a valuable tool in cancer research. Its specific targeting of NAMPT allows for investigations into pathways related to cellular metabolism and cancer cell survival. -
NAMPT Inhibitor
Nampt-IN-9 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis via the enzyme NAMPT. It exhibits significant anticancer activity and has potential applications in research focusing on pancreatic ductal adenocarcinoma. This compound serves as a valuable tool for studying the metabolic pathways and therapeutic strategies related to cancer treatment. -
NAMPT activator
JGB-1-155 is a positive allosteric modulator of nicotinamide phosphoribosyltransferase (NAMPT), displaying an EC50 of 3.29 μM. This compound enhances NAD+ production, thereby mitigating oxidative stress in THP-1 human monocytes. Additionally, JGB-1-155 is effective in reducing TNFα-induced reactive oxygen species (ROS) levels in HT-22 neuronal cells, positioning it as a valuable tool for research into cellular stress responses and metabolic regulation. -
NAMPT Inhibitor
Nampt-IN-13 is a selective inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis through the inhibition of nicotinamide phosphoribosyltransferase (NAMPT). This compound demonstrates significant anti-proliferative effects and is utilized in the study of tumor metabolism and cancer therapy. Its application is particularly relevant in the synthesis of antibody-drug conjugates (ADCs) for targeted cancer treatment research. -
NAMPT Activator
NAMPT activator-7 is a selective activator of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting an EC50 of less than 0.5 μM. This compound effectively enhances NAMPT activity in U2OS cells, promoting NAD+ biosynthesis and potentially supporting cellular metabolism and energy homeostasis. Its applications include research focused on metabolic disorders, cancer biology, and studies related to aging and longevity.
