Catalog No.
Product Name
Application
Product Information
Citations
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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. -
NAMPT Inhibitor
MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), which is often overexpressed in cancer cells to sustain NAD+ levels necessary for rapid cell proliferation. By targeting NAMPT, MS7 serves as a valuable tool for developing PROTAC A7, an effective degrader of NAMPT. This reagent holds significant potential for research applications in cancer biology, particularly in studies focused on metabolic regulation and therapeutic strategies targeting NAMPT. -
NAMPT Inhibitor
Nampt-IN-7 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis by targeting NAMPT, with an IC50 of 7.31 μM. This compound exhibits significant cytotoxicity against the HepG2 hepatocellular carcinoma cell line, demonstrated by an IC50 of 24.28 μM. Nampt-IN-7 is valuable for research applications focusing on cancer metabolism and therapeutic strategies targeting NAD+ synthesis in tumor cells. -
NAMPT Activator
NAMPT activator-6 is a potent activator of nicotinamide adenine monophosphate (NAMPT), playing a crucial role in the regulation of NAD+ biosynthesis. This compound facilitates reversible control over NAMPT and NAD+ levels through light-mediated techniques, enabling the development of photoswitchable proteolysis-targeting chimeras (PS-PROTACs). Research applications include modulation of NAMPT and NAD+ in vivo, offering potential for enhanced antitumor activity while minimizing the side effects associated with traditional inhibitors. -
NAMPT Inhibitor
AS1604498 is a selective competitive inhibitor of human nicotinamide adenine dinucleotide (NAD) biosynthesis enzyme NAMPT, demonstrating an IC50 of 44.4 nM. By inhibiting NAMPT activity, AS1604498 effectively reduces the production of nicotinamide mononucleotide and lowers intracellular NAD levels, leading to the activation of caspase 3/7 and the subsequent induction of apoptosis in cancer cells. This compound is particularly relevant for research focused on chronic myeloid leukemia and related metabolic pathways. -
NAMPT Activator
NAMPT activator-8 is a potent activator of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of less than 0.5 μM. This compound effectively enhances NAMPT activity in U2OS cells, facilitating increased NAD+ synthesis. NAMPT activator-8 is valuable for research applications focused on metabolic regulation and cellular energy homeostasis. -
NAMPT Inhibitor
Nampt-IN-17 is a selective inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis, targeting NAMPT with an IC50 of 17 nM and a Ki of 25.9 nM in human cells. This compound effectively depletes intracellular NAD+ and ATP levels, leading to disrupted mitochondrial membrane potential and subsequently inhibiting cell proliferation, self-renewal, invasion, and migration. Additionally, Nampt-IN-17 induces cell cycle arrest and apoptosis, demonstrating potent selectivity against NAPRT-deficient gastric cancer cells. It serves as a valuable tool for studying the mechanisms underlying NAPRT-deficient gastric cancer. -
PAI-1 Inhibitor
Aleplasinin is a selective inhibitor of SERPINE1 (PAI-1) with an IC50 of 655 nM. By inhibiting PAI-1, Aleplasinin activates the tissue-type plasminogen activator (tPA)/fibrinolysis cascade, facilitating the degradation of amyloid-β (Aβ) oligomers and monomers. This compound has demonstrated significant efficacy in reducing plasma and brain Aβ levels, improving memory function, and reversing cognitive impairment. Aleplasinin is a valuable tool for research focused on Alzheimer’s disease and related neurodegenerative disorders. -
Ser/Thr Protease Inhibitor
ZK824859 hydrochloride is a selective inhibitor of urokinase plasminogen activator (uPA) with a potent IC50 of 79 nM. It also demonstrates varied inhibitory effects on tissue plasminogen activator (tPA) and plasmin, with respective IC50s of 1580 nM and 1330 nM. This compound is particularly relevant for research applications focusing on serine/threonine proteases and their roles in pathological processes, including fibrinolysis and tumor progression. Its oral bioavailability makes it a valuable tool for in vivo studies targeting uPA-mediated pathways. -
PAI-1 Inhibitor
SK-216 is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), playing a crucial role in reducing metastasis in human osteosarcoma. It has demonstrated efficacy in inhibiting lung metastasis associated with this malignancy, making it a valuable compound for research focused on cancer metastasis and therapeutic interventions in osteosarcoma. This compound is suitable for studies exploring the mechanisms of tumor invasion and potential anti-metastatic strategies. -
PAI-1 Inhibitor
CDE-096 is a potent inhibitor of Plasminogen Activator Inhibitor-1 (PAI-1), effectively preventing PAI-1 from inactivating tissue plasminogen activator (tPA) and urokinase plasminogen activator (uPA) with comparable potency (IC50 values of 30 nM and 25 nM, respectively). It demonstrates efficacy against glycosylated forms of PAI-1 and possesses inhibitory activity against PAI-1 derived from various species, including murine, rat, and porcine models, with IC50 values of 19 nM, 22 nM, and 18 nM, respectively. CDE-096 is valuable for research focused on fibrinolysis, thrombolysis, and related cardiovascular studies. -
Angiostatic Agent
Anecortave acetate is a potent ocular angiostatic agent that targets neovascularization. It inhibits angiogenesis driven by various factors and upregulates plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate is valuable in research related to ocular neovascular diseases, facilitating the study of underlying mechanisms and potential therapeutic interventions. -
PAI-1 Inhibitor
Diaplasinin is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), exhibiting an IC50 of 295 nM. This compound demonstrates significant antithrombotic activity, making it valuable for research into coagulation disorders. Its ability to modulate PAI-1 levels may provide insights into therapeutic strategies for conditions associated with thrombosis and fibrinolysis. -
PAI-1 Inhibitor
Toddalolactone is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), demonstrating an IC50 value of 37.31 μM. This compound, derived from Toddalia asiatica, plays a critical role in modulating fibrinolysis and is of significant interest in research related to thrombosis and cardiovascular diseases. Its ability to inhibit PAI-1 activity makes it a valuable tool for investigating pathways involved in clot formation and resolution. -
PAI-1 Inhibitor
AZ3976 is a selective inhibitor of plasminogen activator inhibitor type 1 (PAI-1) that demonstrates an IC50 value of 26 μM in enzymatic chromogenic assays and 16 μM in plasma clot lysis assays. This compound enhances the latency transition of active PAI-1 by reversibly binding to latent PAI-1, thereby facilitating fibrinolysis. AZ3976 is ideal for research applications focused on thrombosis and fibrinolytic processes. -
UK122 TFA Isomer
(E)-UK122 TFA is an isomer of UK122 TFA, functioning as a selective inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 of 0.2 μM. This compound exhibits significant potential in studies related to fibrinolysis and tissue remodeling. Its inhibitory properties make it a valuable tool for research in cancer metastasis and other conditions associated with aberrant plasminogen activation. -
urokinase plasminogen activator Inhibitor
28-O-β-D-Glucopyranosyl pomolic acid is an inhibitor of urokinase plasminogen activator, with an IC50 value of 37.82 μM. This compound can effectively modulate the fibrinolytic pathway by hindering the activation of plasminogen, thereby impacting processes related to fibrin degradation and tissue remodeling. It is suitable for research in fields such as cancer biology, fibrosis, and vascular disorders, where regulation of the uPA system is of significant interest. -
Substrate
D-Val-Leu-Arg-pNA is a substrate for glandular kininoreleasing enzymes and tissue-type plasminogen activator (t-PA), exhibiting no significant affinity for fibrin. This compound is utilized to study enzyme kinetics and the activation mechanisms of proteolytic enzymes involved in various physiological processes. Its specificity for t-PA makes it a valuable tool in research focusing on thrombolytic therapy and related areas. -
Plasminogen Activation Inhibitor
BT-114143 is a plasminogen activation inhibitor, exhibiting an IC50 of 8.42 μM. This compound is valuable in research focused on hemorrhagic diseases stemming from hyperfibrinolysis, including traumatic bleeding, severe menstrual bleeding, postpartum hemorrhage, and complications associated with hemophilia. Its targeted inhibition of plasminogen activation positions it as a potential therapeutic agent in the management of these conditions. -
PAI-1 Inhibitor
XR 5118 hydrochloride is a selective inhibitor of plasminogen activator inhibitor 1 (PAI-1), with an IC50 value of 12 µM. By binding to PAI-1, XR 5118 hydrochloride effectively reduces plasma PAI-1 activity, promoting endogenous thrombolysis and inhibiting thrombus formation. This compound is valuable for research applications related to cancer and thrombotic disorders, providing insights into mechanisms of fibrinolysis and clot regulation. -
Plasmin Substrate
D-Val-Leu-Lys-AMC is a selective fluorogenic peptide substrate for plasmin, enabling the quantification of its enzymatic activity. This compound exhibits increased fluorescence upon cleavage, facilitating studies in fibrinolysis and related processes. It is suitable for applications in enzyme activity assays, offering high sensitivity with excitation at 360-380 nm and emission at 440-460 nm. -
Fibrinolytic Plasminogen Activator
WB 3559 A is a fibrinolytic plasminogen activator that enhances the conversion of plasminogen to plasmin, thereby facilitating the direct degradation of fibrin in thrombus formations. This compound exhibits significant potential in the study of acute thrombotic diseases, such as myocardial infarction and pulmonary embolism, making it a valuable tool for researchers investigating therapeutic strategies in vascular events and clot management. -
PAI-1
D-Val-Leu-Arg-pNA hydrochloride is a specific substrate for plasminogen activator inhibitor-1 (PAI-1). It is utilized to assess the enzymatic activities of plasminogen activators and plasmin. Additionally, this compound is valuable for investigating the fibrinolytic activity in various biological systems, including bacteria and nematodes, facilitating research in thrombosis and clot regulation. -
PCSK9 antagonist
Enlicitide chloride is a potent orally active antagonist of PCSK9, inhibiting the interaction between the lipoprotein lipase (LPL) receptor and PCSK9 with an IC50 of 2.5 nM. This compound is invaluable for investigating cardiovascular diseases, including atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, and acute coronary syndrome, as well as other related cardiometabolic disorders. Researchers may utilize Enlicitide chloride to explore therapeutic strategies targeting lipid metabolism and cardiovascular health. -
PCSK9 Inhibitor
PCSK9-IN-34 is a small molecule inhibitor targeting proprotein convertase subtilisin/kexin type 9 (PCSK9). It plays a crucial role in regulating cholesterol levels by preventing PCSK9-mediated degradation of LDL receptors. This compound is valuable for research into cardiovascular conditions and cholesterol metabolism, particularly in the context of hyperlipidemia and atherosclerosis. -
PCSK9/IDLR/SREBP2 mRNA Inhibitor
5-O-Methylembelin is a natural isocoumarin that functions as an inhibitor of PCSK9, the inducible degrader of the low-density lipoprotein receptor (IDLR), and SREBP2 mRNA expression. This compound is essential for studying lipid metabolism and cholesterol regulation, making it valuable for research focused on hypercholesterolemia and cardiovascular diseases. Its ability to modulate these crucial pathways enables exploration of potential therapeutic strategies targeting lipid homeostasis. -
PCSK9 Inhibitor
PCSK9-IN-10 is a potent oral inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibiting an IC50 value of 6.4 µM. This compound enhances the expression of LDL receptors (LDLR) while downregulating PCSK9 levels, contributing to the reduction of atherosclerosis progression. PCSK9-IN-10 is suitable for research applications focused on hyperlipidemia and cardiovascular diseases. -
PCSK9 Inhibitor
PCSK9-IN-11 is a potent, orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It demonstrates effective transcriptional inhibitory activity in HepG2 cells, with an IC50 value of 5.7 μM. By increasing the protein level of LDL receptors (LDLR), PCSK9-IN-11 serves as a valuable tool for research in atherosclerosis and lipid metabolism. -
PCSK9 inhibitor
PCSK9-IN-23 is a potent inhibitor of PCSK9, effectively blocking its secretion from HepG2 cells. This inhibition leads to a significant increase in LDL receptor (LDLR) expression, making it valuable for research aimed at understanding lipid metabolism and developing therapeutic strategies for hyperlipidemia and cardiovascular diseases. Its ability to modulate LDLR provides insights into cholesterol regulation and potential interventions in related disorders. -
PCSK9 Inhibitor
PCSK9-IN-13 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), significantly disrupting its interaction with low-density lipoprotein (LDL) receptors. With an IC50 value of 537 nM, this compound is instrumental in studying lipid metabolism and cardiovascular diseases. Its application in research can facilitate the development of novel therapeutics for disorders associated with dyslipidemia. -
PCSK9 Inhibitor
SBC-115337 is a potent PCSK9 inhibitor, demonstrating an IC50 value of 0.5 μM. By targeting proprotein convertase subtilisin/kexin type 9 (PCSK9), this compound plays a critical role in modulating cholesterol metabolism. SBC-115337 is suitable for research applications aimed at studying lipid metabolism, cardiovascular diseases, and the development of therapies for hypercholesterolemia. -
PCSK9 Inhibitor
PF-06815345 hydrochloride is a potent, orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), demonstrating an IC50 of 13.4 μM. This compound effectively reduces PCSK9 levels in vivo in mouse models, making it a valuable tool for research into lipid metabolism and cardiovascular disease. Its role as a PCSK9 inhibitor positions it for studies aimed at exploring cholesterol regulation and related therapeutic interventions. -
PCSK9 Inhibitor
PF-06446846 is an orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). This compound selectively targets PCSK9 translation by stalling the 80S ribosome near the codon region, effectively reducing PCSK9 levels. It has significant implications in research related to cholesterol metabolism and cardiovascular diseases, making it a valuable tool for investigations into lipid regulation and associated therapeutic strategies. -
PCSK9 Antagonist
E28362 is a selective PCSK9 antagonist that functions as an orally active lipid-lowering agent. By inhibiting the interaction between PCSK9 and the LDL receptor (LDLR), E28362 promotes the degradation of PCSK9 through the ubiquitin-proteasome pathway, leading to increased cell surface and total levels of LDLR. This mechanism enhances low-density lipoprotein uptake, resulting in significant reductions in plasma lipids, hepatic cholesterol, and triglyceride levels. E28362 also demonstrates minimal cytotoxicity at high concentrations and has been shown to substantially reduce atherosclerotic lesions in animal models, making it a valuable tool in studies of hyperlipidemia and atherosclerosis. -
PCSK9 Inhibitor
PF-06815345 is a potent and orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), exhibiting an IC50 value of 13.4 μM. This compound has been shown to significantly reduce PCSK9 levels in vivo in mouse models. PF-06815345 serves as a valuable tool for studying cholesterol metabolism and the modulation of LDL receptor activity, making it relevant for research in cardiovascular diseases and lipid regulation. -
PCSK9 Inhibitor
7030B-C5 is a potent PCSK9 inhibitor with an IC50 of 1.61 μM. This compound effectively reduces plasma cholesterol and triglyceride levels in vivo, contributing to the attenuation of atherosclerosis progression. 7030B-C5 serves as a valuable tool in cardiovascular disease research, facilitating the exploration of lipid metabolism and associated therapeutic strategies.
