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Catalog No.
Product Name
Application
Product Information
Citations
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MALT1 Protease Inhibitor
MALT1-IN-8 is a potent inhibitor of MALT1 protease, demonstrating an IC50 of 2 nM. This compound effectively inhibits the proliferation of OCI-LY3 lymphoma cells, with an IC50 value of 1.16 μM. MALT1-IN-8 shows potential for anticancer applications, making it a valuable tool for research in lymphoma and other malignancies involving MALT1. -
MALT1 Protease Inhibitor
(R)-MALT1-IN-3 is a selective MALT1 protease inhibitor, exhibiting a potent IC50 of 20 nM. Additionally, this compound demonstrates significant inhibition of interleukin-6 and interleukin-10 with IC50 values of 60 nM and 40 nM, respectively, in OCI-LY3 cells. It serves as a valuable tool for exploring the role of MALT1 in various biological processes, particularly in the context of inflammatory pathways and cancer research. -
MALT1 Protease Inhibitor
MALT1-IN-6 is a selective inhibitor of MALT1 protease, exhibiting a Ki value of 9 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for research focused on cancer therapeutics and the study of signaling pathways modulated by MALT1. Its potency and specificity may facilitate investigations into the roles of MALT1 in various malignancies. -
MALT1 Inhibitor
RGT-068A is a selective and orally bioavailable inhibitor of MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1). This compound demonstrates potent inhibitory activity against MALT1, which is essential for NF-κB signaling in various hematological malignancies and inflammatory diseases. RGT-068A serves as a valuable tool for research into therapeutic strategies targeting MALT1 in cancer and autoimmune disorders. -
MALT1 Protease Inhibitor
MALT1-IN-7 is a potent inhibitor of the MALT1 protease, which plays a crucial role in various oncogenic signaling pathways. Its ability to selectively inhibit MALT1 makes it a valuable tool for investigating the mechanisms underlying cancer development and progression. This compound is particularly relevant for research applications focused on tumor biology and therapeutic strategies targeting MALT1-dependent pathways. -
MALT1 Inhibitor
MALT1-IN-14 is a potent MALT1 inhibitor, exhibiting an IC50 value of 0.081 μM. This compound demonstrates significant inhibition of MALT1's protease activity, making it valuable for studies investigating the role of MALT1 in inflammatory responses and lymphocyte activation. Its application extends to research in various diseases, including hematological malignancies and autoimmune disorders. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
ACOX1 Inhibitor
10,12-Tricosadiynoic acid is a selective and potent inhibitor of acyl-CoA oxidase-1 (ACOX1). It demonstrates significant potential in addressing metabolic disorders induced by high-fat diets or obesity by enhancing mitochondrial lipid metabolism and modulating reactive oxygen species (ROS) levels. Additionally, this compound serves as a versatile click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it valuable for various biochemical applications. -
P2X4 Inhibitor
NP-1815-PX sodium is a selective inhibitor targeting the P2X4 receptor, exhibiting an IC50 of 0.26 μM against human P2X4 receptors. This compound effectively inhibits ATP-mediated prostaglandin production and attenuates TP receptor-induced calcium elevation, as well as NLRP3 inflammasome signaling. Notably, NP-1815-PX sodium demonstrates anti-allodynic effects in vivo and alleviates DNBS-induced colitis symptoms, including weight loss and tissue damage, through the downregulation of IL-1β levels and Caspase-1 activity. This reagent is applicable in research areas such as asthma and inflammatory bowel disease. -
FLAP Inhibitor
Fiboflapon sodium is a potent inhibitor of the 5-lipoxygenase-activating protein (FLAP) with a binding affinity of 2.9 nM. It has an IC50 value of 76 nM for the inhibition of leukotriene B4 (LTB4) in human blood. This compound is valuable in research applications focused on inflammation and related diseases by modulating leukotriene synthesis. Its oral bioavailability makes it suitable for in vivo studies investigating FLAP-related pathways. -
Selective FLAP Inhibitor
Veliflapon is a selective 5-lipoxygenase activating protein (FLAP) inhibitor. This compound effectively inhibits the synthesis of leukotrienes B4 and C4, thereby modulating inflammatory responses. Its primary application lies in research focused on asthma, allergies, and other inflammatory conditions, making it a valuable tool for studying leukotriene-mediated pathways. -
PA2/5-LOX/COX Inhibitor
LY256548 is a potent inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and cyclooxygenase (COX), demonstrating significant anti-ischemic and anti-inflammatory properties. This compound effectively reduces leukotriene B4 production in response to A23187 stimulation. In preclinical models, LY256548 has shown efficacy in mitigating bone damage and paw swelling in rat models of Freund's complete adjuvant-induced arthritis (FCA), making it a valuable tool for research into inflammatory diseases and analgesic mechanisms. -
Leukotriene Receptor/FLAP Inhibitor
(S)-Veliflapon is a potent inhibitor of leukotriene biosynthesis targeting the 5-lipoxygenase activating protein (FLAP). It effectively inhibits the formation of leukotriene B4 (LTB4) in rat, mouse, and human leukocytes with IC50 values of 0.026 µM, 0.039 µM, and 0.22 µM, respectively. Additionally, (S)-Veliflapon demonstrates enantioselectivity in human whole blood, making it a valuable reagent for research in inflammation and related biological processes. -
COX Inhibitor
1-Oxo Ibuprofen is a cyclooxygenase (COX) inhibitor, specifically targeting COX-1 and COX-2 enzymes. As a degradation product and potential impurity of Ibuprofen, it demonstrates significant anti-inflammatory activity with IC50 values of 13 μM for COX-1 and 370 μM for COX-2. This compound is useful for research applications involving the study of prostaglandin synthesis and the metabolic pathways of nonsteroidal anti-inflammatory drugs. -
PKM2 Kinase Inhibitor
PKM2-IN-3 is a selective inhibitor of the PKM2 kinase, demonstrating an IC50 value of 4.1 μM. This compound exhibits notable anti-neuroinflammatory effects by disrupting PKM2-mediated glycolysis and inhibiting NLRP3 activation. PKM2-IN-3 is suitable for research applications focused on metabolic regulation and neuroinflammation pathways. -
G6PD Inhibitor
6-Aminonicotinamide is a competitive inhibitor of glucose-6-phosphate dehydrogenase (G6PD) with a Ki value of 0.46 μM. This powerful antimetabolite of nicotinamide induces ATP depletion, enhancing the efficacy of DNA-crosslinking chemotherapy agents such as Cisplatin. Its ability to modulate metabolic pathways makes it a valuable tool in cancer research and therapeutic applications. -
Nox2 Inhibitor
CPP11G is a selective inhibitor of NADPH oxidase 2 (Nox2), exhibiting an IC50 of 20 μM. This compound is valuable for the investigation of inflammatory diseases, such as vasculitis and atherosclerosis, as well as conditions characterized by Nox2 overactivation, including ischemia-reperfusion injury. Its potential applications in research can aid in understanding the role of Nox2 in various pathological processes. -
Nox Inhibitor
VAS2870 is a selective inhibitor of NADPH oxidase (NOX), primarily targeting NOX1 and NOX2 isoforms. This compound exhibits strong antioxidant properties and effectively reduces reactive oxygen species (ROS) production. VAS2870 is widely utilized in research related to oxidative stress, inflammation, and various pathological conditions associated with NOX activity. -
NOX1/4 Inhibitor
GKT136901 is a selective and orally active inhibitor of NADPH oxidases NOX1 and NOX4, exhibiting inhibition constants (Kis) of 160 nM and 165 nM, respectively. This compound also serves as a direct scavenger of peroxynitrite, contributing to its anti-inflammatory properties. GKT136901 is particularly useful in research focused on diabetic nephropathy, stroke, and neurodegenerative diseases, providing valuable insights into oxidative stress-related pathologies. -
Nox1 Inhibitor
NoxA1ds is a selective inhibitor of NADPH oxidase 1 (NOX1), with an IC50 of 20 nM. It effectively inhibits NOX1-derived superoxide production in HT-29 human colon cancer cells. Additionally, NoxA1ds reduces VEGF-induced migration of human pulmonary artery endothelial cells under hypoxic conditions in vitro. This reagent is valuable for research into hypertension, atherosclerosis, and cancer biology. -
Nox Inhibitor
NADPH oxidase-IN-1 is an orally active inhibitor of NADPH oxidase (Nox), specifically targeting Nox2 and Nox4 with IC50 values of 1.9 μM and 2.47 μM, respectively. This compound is notable for its ability to penetrate the blood-brain barrier, making it relevant for studies involving neuronal inflammation. NADPH oxidase-IN-1 effectively suppresses the production of pro-inflammatory cytokines and inhibits LPS-mediated microglial migration, demonstrating promising in vivo efficacy for potential therapeutic applications in neuroinflammatory conditions. -
NOX1/4 Inhibitor
GKT136901 hydrochloride is a highly selective and orally active inhibitor of NADPH oxidase isozymes NOX1 and NOX4, exhibiting inhibition constants of 160 nM and 165 nM, respectively. This compound also functions as a direct scavenger of peroxynitrite, enhancing its therapeutic potential. GKT136901 hydrochloride is primarily utilized in research settings focusing on diabetic nephropathy, stroke, and neurodegenerative diseases, while also demonstrating notable anti-inflammatory properties. -
Nox2/4 Inhibitor
GLX481304 is a selective inhibitor of Nox2 and Nox4, exhibiting an IC50 of 1.25 μM. This compound effectively suppresses reactive oxygen species (ROS) production in isolated mouse cardiomyocytes and enhances cardiac contractility. GLX481304 is applicable in research focused on ischemic heart injury, providing valuable insights into oxidative stress-related pathophysiology. -
NOX1 Inhibitor/ROS Inhibitor
Fluoflavine is a selective inhibitor of NOX1 and reactive oxygen species (ROS) production. This compound effectively reduces ROS levels, NOX1-mediated signaling pathways, and prevents retinal ganglion cell death induced by oxygen-glucose deprivation. In preclinical studies, Fluoflavine has demonstrated the ability to inhibit NADPH oxidase activity and mitigate pathological retinal neovascularization in models of oxygen-induced retinopathy. It is a valuable tool for investigating retinal ischemia-reperfusion injury and proliferative retinopathy. -
NOX2 Inhibitor
NOX2-IN-2 diTFA is a potent inhibitor of NOX2, specifically targeting the p47phox-p22phox protein-protein interaction with a Ki of 0.24 μM. This compound effectively inhibits reactive oxygen species (ROS) production derived from NOX2 in cellular environments. It is valuable for research applications focused on oxidative stress and related signaling pathways. -
NADPH Oxidase Inhibitor
NOX2-IN-3 is a selective inhibitor of NADPH Oxidase 2 (NOX2). This compound has been shown to enhance the sensitivity of tumor cells to MRTX1133, indicating its potential role in cancer research. NOX2-IN-3 may be valuable for studies focused on oxidative stress and its implications in tumor biology. -
CBR1 Inhibitor
YF-Mo1 is a selective inhibitor of the carbonyl reductase 1 (CBR1), exhibiting an IC50 value of 1.1 μM. This compound demonstrates potential in modulating CBR1 activity, which is significant in metabolic processes and drug metabolism. YF-Mo1 is valuable for research exploring the role of CBR1 in various physiological and pathological conditions, offering insights into metabolic therapies and drug interactions. -
NQO1 Inhibitor
N-Benzyl-N-demethylpronqodine A is an inhibitor of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1), exhibiting an IC50 value of 83.3 nM. This compound plays a significant role in the study of redox biology and the mechanisms of cellular response to oxidative stress. Its application includes investigating the implications of NQO1 inhibition in various disease models, facilitating research in cancer biology and drug metabolism. -
NOX2 Inhibitor
NOX2-IN-2 is a potent inhibitor of NOX2, specifically targeting the p47phox-p22phox protein-protein interaction with a Ki of 0.24 μM. This compound effectively reduces reactive oxygen species (ROS) production mediated by NOX2 in cellular contexts. NOX2-IN-2 is ideal for research applications focused on oxidative stress, inflammation, and related signaling pathways. -
ALK Inhibitor
TSR-011-isomer is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 6 nM. This compound demonstrates significant biological activity by undergoing metabolic hydrolysis and NADPH-dependent metabolism, facilitating its clearance in biological systems. TSR-011-isomer is suitable for research focused on ALK-driven cancers, making it a valuable tool for studies in cancer biology and targeted therapy development. -
CBR1 Inhibitor
CBR1-IN-3 is a potent inhibitor of carbonyl reductase 1 (CBR1), exhibiting an IC50 value of 0.034 μM. This compound serves as a valuable research tool for studies focusing on the modulation of carbonyl metabolites in various biological systems. Its ability to effectively inhibit CBR1 makes it suitable for investigating the enzyme's role in drug metabolism and potential therapeutic applications. -
NADPH Oxidase Inhibitor
Diapocynin, a dimeric derivative of Apocynin, functions as a potent NADPH oxidase inhibitor. This compound exhibits significant anti-inflammatory, neuroprotective, and antioxidant activities, making it valuable for research into oxidative stress, neurodegenerative diseases, and inflammation-related conditions. Its oral bioavailability enhances its utility in various experimental settings aimed at understanding the role of reactive oxygen species in cellular processes. -
NOX2 Inhibitor
NOX2-IN-1 is a selective inhibitor of nicotinamide adenine dinucleotide phosphate oxidase isoform 2 (NOX2). It effectively disrupts the protein-protein interaction between p47phox and p22phox, demonstrating favorable binding affinities and significant cellular activity. This compound is valuable for research applications focusing on oxidative stress-related diseases and inflammation pathways. -
NOX1 Inhibitor
ML171 analog 1 is a selective inhibitor of NOX1, a member of the NADPH oxidase family implicated in various cellular processes. This compound exhibits significant biological activity in the modulation of reactive oxygen species, making it a valuable tool in cancer research. Its role in inhibiting NOX1 provides insights into oxidative stress related pathways in tumor biology. -
Thrombin Inhibitor
PPACK dihydrochloride is a potent and selective irreversible inhibitor of thrombin. It serves as an alternative anticoagulant to lithium heparin for blood gas and electrolyte analyses in whole blood. Additionally, PPACK dihydrochloride inhibits plasminogen activator (rt-PA), preventing its binding to plasma protease inhibitors. This compound also reduces plasmin-induced endothelial permeability and morphological changes in bovine aortic endothelial cell monolayers, making it suitable for investigations in thrombosis-related research. -
PPT1 Inhibitor
Ezurpimtrostat (hydrochloride) is a potent and selective PPT1 inhibitor with multiple biological activities. It disrupts lysosomal function, modulates autophagy, and induces apoptosis, making it a valuable tool in cancer research and immunology. This compound has demonstrated efficacy in reducing inflammatory markers such as IFN-α and CRP, as well as in lowering viral loads of SARS-CoV-2. Ezurpimtrostat is suitable for investigating conditions such as systemic lupus erythematosus, hepatocellular carcinoma, fibrosis, and other related disorders. -
FAP Inhibitor
BR102910 is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 2 nM. Additionally, BR102910 exhibits inhibition of prolyl oligopeptidase (PREP) with an IC50 of 49.00 μM. This compound is primarily used in research focusing on type 2 diabetes and related metabolic disorders, making it a valuable tool for exploring FAP's role in these conditions. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-7 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), exhibiting an IC50 value of 0.45 µM. This compound plays a crucial role in modulating the Nrf2 signaling pathway, which is essential for cellular responses to oxidative stress. Its application is significant in studies focused on neuroprotection, cancer therapy, and various diseases associated with oxidative damage. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-23 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting an IC50 of 16.0 nM. It demonstrates strong binding affinity to Keap1 with a Kd value of 3.07 nM, making it a valuable tool for research into antioxidant response pathways. This compound is suitable for studies related to cellular defense mechanisms and may have applications in the field of cancer research and neurodegenerative diseases. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-3 is a selective inhibitor targeting the KEAP1-NRF2 protein-protein interaction, demonstrating a Kd value of 2.5 nM for KEAP1. This compound enhances NRF2 activity, leading to elevated expression of antioxidant response genes. It is valuable for research applications focused on oxidative stress, cancer biology, and neuroprotection, providing insights into mechanisms influencing cellular defense pathways. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-28 is a potent inhibitor of the Keap1-Nrf2 signaling pathway. This compound exhibits significant antioxidant activity by promoting the upregulation of Nrf2 and its downstream targets, including HO-1, GCLM, and Akr1c1. Additionally, Keap1-Nrf2-IN-28 has been shown to mitigate acute liver injury induced by acetaminophen, making it a valuable tool in research related to oxidative stress and liver protection. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-5 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), with an IC50 of 4.1 µM and a Kd of 3.7 µM. This compound enhances Nrf2 activity, promoting the expression of antioxidant and cytoprotective genes. It serves as a valuable tool for research into oxidative stress, neuroprotection, and cancer therapeutics. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-8 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, demonstrating IC50 values of 64.5 nM and 14.2 nM in fluorescence polarization and time-resolved fluorescence resonance energy transfer assays, respectively. This compound effectively enhances the mRNA expression of key Nrf2 target genes, including GSTM3, HMOX2, and NQO1. Keap1-Nrf2-IN-8 is instrumental in research focused on oxidative stress response and cellular defense mechanisms. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-15 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting IC50 values of 77 nM in fluorescence polarization (FP) assays and 2.5 nM in time-resolved Förster resonance energy transfer (TR-FRET) assays. This compound enhances the activation of the Nrf2 pathway, which plays a critical role in cellular defense mechanisms against oxidative stress and inflammation. Keap1-Nrf2-IN-15 is a valuable tool for research applications focused on neuroprotection, cancer therapy, and the modulation of antioxidant responses. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-12 is a potent inhibitor of the Keap1-Nrf2 interaction, exhibiting an IC50 value of 2.30 µM. This compound effectively modulates the Nrf2 signaling pathway, which is critical for cellular defense against oxidative stress. Additionally, Keap1-Nrf2-IN-12 demonstrates metabolic stability in human liver microsomes, making it a valuable tool for research applications focused on oxidative stress response and related therapeutic targets. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-22 is a selective inhibitor of the Keap1-Nrf2 interaction, exhibiting a KD2 value of 42.2 nM for Keap1. This compound is valuable for investigating the regulatory mechanisms of oxidative stress and cytoprotection in cellular environments. Key research applications include the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury, where modulation of the Nrf2 pathway may provide therapeutic insights. -
KEAP1 Inhibitor
Keap1-IN-2 is a potent KEAP1 inhibitor with an IC50 of 2 nM, designed to indirectly activate Nrf2. By inhibiting KEAP1, this compound enhances cellular antioxidant capacity and promotes the accumulation and nuclear translocation of Nrf2, preventing its degradation. Keap1-IN-2 is applicable in research exploring diseases linked to oxidative stress, including inflammatory bowel disease, Crohn's disease, and immune disorders such as ulcerative colitis. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-17 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction. This compound enhances the activation of the Nrf2 pathway, which plays a critical role in cellular defense against oxidative stress and inflammation. Keap1-Nrf2-IN-17 is valuable for research applications focused on understanding the mechanisms of oxidative stress response and exploring therapeutic options for related diseases. -
NF-κB Inhibitor
NF-κB-IN-4 is a potent inhibitor of the NF-κB signaling pathway, demonstrating significant blood-brain barrier permeability. This compound exhibits anti-neuroinflammatory activity through its ability to block the phosphorylation and activation of IκBα, thereby reducing NLRP3 expression and inhibiting NF-κB activation. NF-κB-IN-4 is suitable for research applications related to neuroinflammatory diseases, providing a valuable tool for therapeutic investigations. -
BChE Inhibitor
S21-1011 is a selective inhibitor of butyrylcholinesterase (BChE) with IC50 values of 0.059 μM for equine BChE and 0.162 μM for human BChE. This compound demonstrates effective blood-brain barrier permeability and favorable pharmacokinetic properties. Additionally, S21-1011 exhibits anti-inflammatory activity by activating the keap1-Nrf2-ARE signaling pathway, with an EC50 of 23.48 μM for antioxidant response element activation. Its potential to ameliorate cognitive impairments in murine models of Alzheimer’s disease makes it relevant for neurodegenerative research applications.
