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Lipoxygenase Inhibitor
Aureusidin is a potent lipoxygenase inhibitor known for its significant antioxidant properties. It exhibits anti-inflammatory effects, making it a valuable compound for research focused on inflammatory pathways and oxidative stress responses. Aureusidin is applicable in studies investigating the modulation of lipoxygenase activity and its implications in various diseases. -
Neuroprotective Agent
Leteprinim potassium (AIT-082) is a purine analog that functions as a neuroprotective agent. This compound enhances cognitive function by promoting the production of brain-derived neurotrophic factor (BDNF) mRNA in response to spinal cord injuries, and nerve growth factor (NGF) mRNA in the basal forebrain. Additionally, Leteprinim potassium mitigates glutamate-induced toxicity in cultured hippocampal neurons and elevates the mRNA levels of heme oxygenase 1 and 2, contributing to cellular defense against reactive oxygen species. Its applications extend to research on neuroprotection and cognitive enhancement strategies. -
Endogenous Metabolite
Succinyl phosphonate is a selective inhibitor of α-ketoglutarate dehydrogenase (KGDHC) and 2-oxoglutarate dehydrogenase (OGDH). It effectively inhibits KGDHC activity in various cell types including muscle, bacterial, brain, and cultured human fibroblasts, demonstrating distinct effects on cell viability influenced by metabolic conditions in cancer cells. Additionally, succinyl phosphonate trisodium salt is known to reduce glutamate-induced reactive oxygen species (ROS) production in glutamate-stimulated hippocampal neurons, making it a valuable tool for studies in metabolic pathways and neurotoxicity. -
Herbicide
Topramezone is a selective inhibitor of 4-hydroxyphenylpyruvate dioxygenase (4-HPPD), functioning primarily as a herbicide. This compound demonstrates effective post-emergence control of broadleaf and grass weeds in corn crops, making it valuable for agricultural research and herbicide efficacy studies. Its mechanism of action targets specific pathways in the weed species, offering insights into weed resistance management and the development of sustainable agrochemical practices. -
Monoamine Oxidase Inhibitor
Nialamide hydrochloride is a non-selective monoamine oxidase (MAO) inhibitor. It effectively inhibits MAO, regulating reactive oxygen species (ROS) production and influencing various physiological responses. This compound induces hyperkinesis in animal models, enhances the anticonvulsant effects of Diphenylhydantoin in mice, and increases rectal temperature while augmenting the pressor response to Norepinephrine. Nialamide hydrochloride is valuable in research focused on depression, inflammatory diseases, neurodegenerative disorders, and hypertension. -
Photosensitizer
Benz-AP is a potent photosensitizer that generates singlet oxygen, exhibiting a negative correlation with human carboxylesterase 2 (hCES2) activity. This compound demonstrates enhanced photocytotoxicity in cancer cells, particularly in environments with low hCES2 levels. Upon two-photon excitation (TPE), Benz-AP produces reactive oxygen species (ROS), effectively inducing cell death in cancer cells and tumor spheroids, making it a valuable tool for cancer research applications. -
α-Glucosidase Inhibitor
Guavinoside B is an orally active α-glucosidase inhibitor, exhibiting an IC50 of 0.21 mM. It demonstrates significant biological activity by upregulating the expressions of Nrf2, GCLC, and NQO1 while downregulating p-JNK expression and reducing intracellular reactive oxygen species levels. Guavinoside B effectively decreases serum TNF-α levels associated with Acetaminophen, alleviating hepatocellular infiltration and necrosis, and improving liver-related biochemical parameters. This compound is relevant for research in diabetes and Acetaminophen-induced liver injury. -
IDO Inhibitor
Pronqodine A is an inhibitor of Indoleamine 2,3-Dioxygenase (IDO) with an IC50 of 131.5 nM. It effectively reduces bradykinin-induced release of PGE2, 6-keto-prostaglandin F1α, and PGD2, while simultaneously inducing reactive oxygen species (ROS) production in human synovial sarcoma SW982 cells. Additionally, Pronqodine A serves as a substrate for human quinone reductase NQO1, making it a valuable tool for research into inflammation and related biological processes. -
hMAO-B Inhibitor
CHBO4 is a potent, reversible, competitive inhibitor of human monoamine oxidase B (hMAO-B), with an IC50 value of 0.031 μM and a Ki value of 0.010 ± 0.005 μM. This compound demonstrates the ability to reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 is suitable for research applications focused on Parkinson's disease (PD) and related neurodegenerative conditions. -
Antioxidant
1,2-Diacetoxy-4,7,8-trihydroxy-3-(4-hydroxyphenyl)dibenzofuran is an antioxidant compound derived from the edible mushroom Sarcodon leucopus. It exhibits significant free radical scavenging activity, demonstrated by an IC50 of 28 μM in the DPPH assay. Additionally, it effectively inhibits malondialdehyde (MDA) formation with an IC50 of 71 μM and α-glucosidase activity with an IC50 of 6.22 μM, making it a valuable reagent for studies in antioxidant research and metabolic disorders. -
MAO-B Inhibitor
MAO-B-IN-7 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE), demonstrating IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. This compound is notable for its ability to penetrate the blood-brain barrier, making it suitable for central nervous system research. MAO-B-IN-7 has been shown to mitigate oxidative stress and neuroinflammation, supporting its potential applications in neurodegenerative disease studies. -
Enantiomer
(3S,4R)-ME-344 is a selective inhibitor of mitochondrial heme oxygenase 1 (HO-1) that functions by binding to and modifying the structure of HO-1. This enantiomer promotes the translocation of HO-1 from the rough endoplasmic reticulum to the mitochondria specifically in drug-sensitive cell lines such as H460 and SHP-77. By decreasing mitochondrial ATP production and inducing reactive oxygen species (ROS), it disrupts redox homeostasis and mitochondrial function. With its notable antitumor activity, (3S,4R)-ME-344 is a valuable compound for research in cancer, including studies focused on breast cancer. -
MAO-B Inhibitor
MAO-B-IN-54 is a selective, reversible, and competitive inhibitor of monoamine oxidase B (MAO-B), exhibiting a human IC50 of 0.052 μM and a Ki of 0.028 μM. This compound demonstrates minimal activity against MAO-A and effectively binds to both the entrance and substrate cavity of MAO-B, establishing hydrophobic and hydrogen bonding interactions. MAO-B-IN-54 has been shown to inhibit amyloid-beta (Aβ) aggregation and reduce reactive oxygen species (ROS) production, making it a valuable tool for research into Alzheimer's disease mechanisms. -
Herbicide
Bifenox is a nitrophenyl ether herbicide that primarily targets and disrupts cellular membranes while inhibiting photosynthesis and protoporphyrinogen oxidase activity. This compound is known to significantly increase reactive oxygen species (ROS) production in the microalga Chlamydomonas reinhardtii. Its biological activity makes Bifenox a valuable reagent for research in plant physiology and herbicide mechanisms. -
MAO-B Inhibitor
Sembragiline is a potent and selective reversible inhibitor of monoamine oxidase B (MAO-B). By inhibiting MAO-B activity, Sembragiline decreases the metabolism of dopamine and other amine neurotransmitters, potentially increasing their levels within the brain. This inhibition also reduces the formation of toxic reactive oxygen species (ROS), which are implicated in the pathology of Alzheimer's disease (AD). Sembragiline demonstrates favorable oral bioavailability and effective permeability across the blood-brain barrier, making it a valuable tool for research on AD, particularly in patients exhibiting elevated MAO-B activity. -
MAO-B Inhibitor
MAO-B-IN-49 is a selective and reversible inhibitor of monoamine oxidase B (MAO-B), with an impressive IC50 of 1 nM for human MAO-B and minimal activity against MAO-A (IC50 = 633.9 μM). This compound effectively reduces reactive oxygen species (ROS) production in HT22 cells, demonstrating substantial neuroprotective effects. In preclinical models of Parkinson's disease, MAO-B-IN-49 significantly mitigates motor dysfunction in MPTP-induced mice, making it a valuable reagent for studying neurodegenerative disorders and their underlying mechanisms. -
α-Amylase Inhibitor
α-Amylase-IN-14 is a selective inhibitor of α-amylase, demonstrating robust interactions with the enzyme (-5.55 kcal/mol). This compound serves as a dual anti-inflammatory and anti-hyperglycemic agent, exhibiting significant radical scavenging activity against DPPH and ABTS radicals. α-Amylase-IN-14 is valuable for research focused on diabetes and related metabolic disorders. -
Fungal Metabolite
Fusarochromanone, a fungal metabolite, primarily targets the JNK signaling pathway. It exhibits significant anti-angiogenic and anti-cancer properties, likely mediated by the induction of reactive oxygen species (ROS). This compound is valuable in cancer research and therapeutic development, particularly in studies focusing on angiogenesis and oxidative stress responses. -
Antioxidant
Tricetinidin chloride is an antioxidant that targets oxidative stress. It exhibits protective effects on rat renal cells by reducing reactive oxygen species (ROS) production, enhancing glutathione (GSH) levels, restoring mitochondrial membrane potential, and upregulating heme oxygenase-1 (HO-1) expression. Additionally, Tricetinidin chloride inhibits the expression of immunoglobulin E (IgE) receptors on human mast cells, making it a valuable tool for researching inflammatory and allergic diseases. -
MAO-B Inhibitor
Multi-target kinase-IN-10 is a selective and reversible inhibitor of monoamine oxidase B (MAO-B), exhibiting an IC50 of 0.0053 μM. This compound effectively penetrates the blood-brain barrier and competitively binds to the active site of MAO-B, disrupting substrate interactions. By chelating Cu2+ ions, it inhibits copper-induced reactive oxygen species (ROS) production and decreases the release of pro-inflammatory cytokines such as NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 holds potential for therapeutic applications in the treatment of Parkinson's disease. -
Stable Isotope
Sulforaphane-d8 is a deuterium-labeled derivative of sulforaphane, targeting the Keap1/Nrf2/ARE signaling pathway. This compound is an effective inducer of tumor-suppressing proteins and has been shown to inhibit histone deacetylase (HDAC) activity. Sulforaphane-d8 provides cardioprotective effects by enhancing heme oxygenase-1 (HO-1) expression and has demonstrated potential in suppressing high glucose-induced pancreatic cancer through AMPK-dependent signaling. This reagent is valuable for anticancer and anti-inflammatory research applications. -
Anticancer Agent
Thiabenzanilide 63T is a small molecule anticancer agent that selectively triggers cancer cell death through a caspase-independent pathway. It generates reactive oxygen species and promotes lipid peroxidation, exhibiting strong cytotoxic effects against lung-derived cancer cell lines. Additionally, Thiobenzanilide 63T significantly reduces the expression of heme oxygenase (HO-1) in A549 cells, making it valuable for research in cancer biology and therapeutic development. -
PPARγ Inhibitor, heme oxygenase-1 Activator, Nrf2 Activator
PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders. -
Reactive Oxygen Species Inhibitor
Heme Oxygenase-1-IN-2 is a selective inhibitor of heme oxygenase-1, exhibiting an IC50 of 0.95 μM. This compound demonstrates significant antiproliferative activity in vitro, making it a valuable tool in the study of reactive oxygen species and their roles in cellular processes. Its application extends to research involving oxidative stress and potential therapeutic interventions in various diseases related to dysregulated oxidative pathways. -
HO Inhibitor
N'-Isonicotinoylisonicotinohydrazide is a competitive inhibitor of heme oxygenase (HO), demonstrating an IC50 range of 5-30 μM. This compound significantly impedes iron release, thereby disrupting iron acquisition in bacteria. It exhibits selective inhibitory effects on HO enzymes from Pseudomonas aeruginosa and Neisseria meningitidis, making it a valuable tool for investigating multidrug-resistant Gram-negative bacterial infections. -
Heme oxygenase-1 Inducer
HIF-PHD-IN-3 is a potent inducer of heme oxygenase-1 (HO-1) through inhibition of hypoxia-inducible factor prolyl hydroxylases (HIF-PHDs). This compound exhibits cardioprotective properties, making it valuable in research focused on cardiac cell survival and stress responses. HIF-PHD-IN-3 is primarily utilized in studies investigating the role of HO-1 in cardiovascular health and various pathophysiological conditions. -
Pancreatic Lipase/Acetylcholinesterase/Glutamic-oxaloacetic Transaminase 1/Alpha-glucosidase Inhibitor
Aspulvinone H is a potent inhibitor targeting pancreatic lipase, acetylcholinesterase, glutamic-oxaloacetic transaminase 1 (GOT1), and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It demonstrates key biological activities including inhibition of cancer cell proliferation, disruption of glutamine metabolism, and induction of apoptosis in cancer cells. Additionally, Aspulvinone H lowers postprandial blood glucose levels in mice and exhibits antibacterial properties against Staphylococcus aureus. This compound is suitable for research into pancreatic ductal adenocarcinoma, diabetes management, and infectious diseases caused by Staphylococcus aureus. -
HO-1 Inhibitor
Dehydrocurdione, a sesquiterpene derived from zedoary, acts as a heme oxygenase-1 (HO-1) inhibitor. It is known to induce the expression of HO-1 in RAW 264.7 macrophages through interaction with Keap1, leading to the translocation of Nrf2 and activation of the HO-1 E2 enhancer. Additionally, Dehydrocurdione demonstrates anti-inflammatory properties by suppressing lipopolysaccharide-induced nitric oxide release, marking its potential application in research related to inflammation and oxidative stress. -
HO-1/HO-2 Inhibitor
Azalanstat is an imidazole-dioxolane derivative that functions as a specific inhibitor of heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2), with IC50 values of 5.5 µM and 24.5 µM, respectively. This compound is valuable for studying the roles of HO-1 and HO-2 in various biological processes, including inflammation and oxidative stress. Its inhibition properties make Azalanstat a useful tool in research focused on diseases where the modulation of heme oxygenase activity is relevant. -
FXR Inhibitor
Gly-β-MCA is a potent farnesoid X receptor (FXR) inhibitor, selectively acting within the intestine. This stable bile acid demonstrates significant biological activity, making it a promising candidate for research focused on metabolic disorders. Its oral bioavailability enhances its potential for therapeutic application and further investigation in related studies. -
Endogenous Metabolite
Moracin M is a phenolic compound derived from Mori Cortex that acts as a potent inhibitor of phosphodiesterase-4 (PDE4), exhibiting IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research in inflammation and related signaling pathways. Its potential applications include studying the role of PDE inhibition in various disease models. -
Endogenous Metabolite
Meglutol is an endogenous metabolite that functions as a lipid-lowering agent by inhibiting HMG-CoA reductase, a key enzyme in cholesterol biosynthesis. It effectively reduces levels of cholesterol, triglycerides, serum β-lipoprotein, and phospholipids. Additionally, Meglutol is noted for inducing significant lipid oxidative damage in brain tissue, making it a valuable tool for research in cardiovascular and metabolic diseases. -
Endogenous Metabolite
Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that predominantly activates farnesoid X receptor (FXR), a nuclear receptor integral to cholesterol metabolism and homeostasis. This compound plays a significant role in regulating lipid metabolism and has been implicated in therapeutic applications related to metabolic disorders, particularly in studies investigating the modulation of bile acid signaling pathways. Its ability to influence liver function and glucose metabolism makes it a valuable reagent in biological research focused on metabolic regulation and associated pathologies. -
Foxo1 Inhibitor
AS1708727 is an orally active inhibitor of Foxo1, exhibiting EC50 values of 0.33 μM for glucose-6-phosphatase (G6Pase) and 0.59 μM for phosphoenolpyruvate carboxykinase (PEPCK). This compound plays a significant role in modulating metabolic pathways and is valuable for research into glucose homeostasis and metabolic disorders. AS1708727 can be utilized in studies investigating the therapeutic potential of targeting Foxo1 in various diseases, including diabetes and cancer. -
RAR Agonist
Retinoic acid-d5 is a deuterium-labeled derivative of retinoic acid, functioning as a selective retinoic acid receptor (RAR) agonist. It is crucial for cellular processes such as growth, differentiation, and organogenesis, demonstrating IC50 values of 14 nM for RARα, β, and γ subtypes. Additionally, retinoic acid-d5 interacts with the peroxisome proliferator-activated receptor β/δ (PPARβ/δ) with a Kd of 17 nM and inhibits the transcription factor Nrf2 through RARα activation. This compound is essential for studies involving retinoid signaling and cell differentiation. -
HMG-CoA Reductase Inhibitor
Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor that effectively reduces blood lipid levels. This compound demonstrates the ability to inhibit human smooth muscle cell proliferation and invasion, with IC50 values of 0.39 μM and 2.39 μM, respectively. Its capacity to modulate lipid metabolism makes it significant for research in cardiovascular diseases and metabolic disorders. -
FAAH Inhibitor
Macamide B is a selective inhibitor of fatty acid amide hydrolase (FAAH), derived from the plant Lepidium meyenii. This compound has been shown to enhance levels of endocannabinoids by inhibiting their degradation, thereby playing a crucial role in modulating pain and inflammation. Macamide B is primarily utilized in research focused on pain management, neuroprotection, and the therapeutic potential of endocannabinoids in various physiological processes. -
12R-LOX Inhibitor
12R-LOX-IN-2 is a potent inhibitor of 12R-lipoxygenase (12R-LOX), demonstrating significant biological activity in the modulation of keratinocyte proliferation. This compound effectively inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and suppresses colony formation. Additionally, 12R-LOX-IN-2 decreases protein levels of Ki67 and mRNA expression of IL-17A in IMQ-treated cells, making it a valuable reagent for research on psoriasis and related skin inflammatory conditions. -
Ser/Thr Protease Inhibitor
Antipain is a serine/threonine protease inhibitor derived from Actinomycetes. It exhibits significant biological activity by inhibiting N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced cellular transformation and promoting chromosomal aberrations. Additionally, Antipain has been shown to impair uterine DNA synthesis and function in murine models, making it a valuable reagent for studies related to cellular transformation, DNA damage response, and reproductive biology. -
CYP2C19 Inhibitor
CYP2C19-IN-1 is a selective inhibitor of the cytochrome P450 enzyme CYP2C19, exhibiting a favorable safety profile with no hepatotoxicity or Ames test toxicity. It demonstrates potent inhibition of RNA-dependent RNA polymerase (RdRP) with a Ki value of 6.16 µM. This compound is primarily utilized in research focused on antiviral therapies against Zika virus (ZIKV). -
12R-LOX Inhibitor
12R-LOX-IN-1 is a selective inhibitor of 12-lipoxygenase (12R-LOX), with an IC50 of 28.25 μM. This compound effectively reduces the hyper-proliferative state and colony-forming ability of Imiquimod-induced psoriatic keratinocytes. Additionally, 12R-LOX-IN-1 modulates key inflammatory markers by inhibiting the production of reactive oxygen species, Ki67, IL-17A, TNF-α, and IL-6. It is a valuable tool for antipsoriatic research and the investigation of related biological pathways. -
DHFR Inhibitor
Trimetrexate isethionate is a potent dihydrofolate reductase (DHFR) inhibitor, effectively reducing DNA and RNA precursor synthesis, which leads to cytotoxicity. With IC50 values of 4.74 nM for human DHFR and 1.35 nM for Toxoplasma gondii DHFR, it demonstrates significant antimicrobial and antitumor activity. This compound is valuable for research applications targeting Pneumocystis carinii pneumonia (PCP) and various cancer types. -
DHFR Inhibitor
Trimetrexate trihydrochloride is a potent dihydrofolate reductase (DHFR) inhibitor that effectively reduces the synthesis of DNA and RNA precursors, leading to cell death. With IC50 values of 4.74 nM for human DHFR and 1.35 nM for Toxoplasma gondii DHFR, this compound demonstrates strong inhibitory activity. Trimetrexate trihydrochloride is utilized in research focused on Pneumocystis carinii pneumonia (PCP) and various cancer cell types, offering valuable insights into therapeutic applications. -
TbNMT Inhibitor
DDD100097 is a potent inhibitor of the N-myristoyltransferase enzyme (TbNMT), exhibiting an IC50 value of 2 nM. This compound enhances blood-brain barrier permeability, making it a valuable tool in the investigation of therapeutic approaches for African trypanosomiasis. DDD100097 is suitable for research applications focused on the modulation of trypanosome biology and treatment strategies. -
PDE4B Inhibitor
Nerandomilast is a potent inhibitor of phosphodiesterase 4B (PDE4B) with an IC50 value of 7.2 nM. Its oral bioavailability and favorable safety profile make it a valuable tool in the research of inflammatory conditions, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD). This compound may facilitate the development of novel therapeutic strategies targeting PDE4B-mediated pathways. -
PDE2A Inhibitor
PDM-631 is a selective inhibitor of phosphodiesterase type 2A (PDE2A) that is both orally active and capable of penetrating the blood-brain barrier. This compound demonstrates potent inhibitory effects, with IC50 values of 1.5 nM against human recombinant PDE2A and 4.2 nM against rat recombinant PDE2A. PDM-631 reliably elevates cGMP levels in the rat cerebral cortex and is valuable for investigating schizophrenia and various neurodegenerative disorders. -
PDE4/PDE IV Inhibitor
Ro 20-1724 is a selective inhibitor of cAMP-specific phosphodiesterase 4 (PDE4). With a Ki value of 1930 nM, it effectively enhances cAMP levels, contributing to its neuroprotective properties. This compound is primarily utilized in research applications focused on neurobiology and the modulation of inflammatory responses. -
PDE3/PDE4 Inhibitor
Ensifentrine is a potent dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), exhibiting IC50 values of 0.4 nM and 1479 nM, respectively. By inhibiting these enzymes, Ensifentrine elevates the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, leading to bronchodilation and reduced activation and migration of inflammatory cells. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD). -
PDE5 Inhibitor
Zaprinast is a selective inhibitor of cGMP-selective Phosphodiesterase 5 (PDE5), leading to a notable increase in cGMP levels in cardiac myocytes. In addition to its PDE5 inhibition, Zaprinast acts as an agonist for G protein-coupled receptor 35 (GPR35), demonstrating strong activation in rat models and moderate activation in human models. This compound exhibits antiproliferative and proapoptotic effects, making it valuable for research applications focused on vascular remodeling and related cardiovascular studies. -
PDE4 Activator
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), specifically targeting PDE4A4, PDE4B1, PDE4C3, and PDE4D5 variants. This compound effectively inhibits PGE2-induced cyst formation in MDCK cells, exhibiting an EC50 of 1.2 μM. MR-L2 serves as a valuable tool for studying PDE4-related signaling pathways and exploring potential therapeutic applications in conditions involving dysregulated PDE4 activity.

