Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Drug Metabolite
Cyslopentenyl cytosine triphosphoric is a bioactive metabolite of the nucleoside analogue cyclopentenyl cytosine (CPEC) that primarily targets CTP synthetase. This compound effectively inhibits CTP synthetase activity, leading to a depletion of cytidine nucleotide pools. Cyslopentenyl cytosine triphosphoric is essential for research into cancer biology, particularly in the study of leukemia and other related malignancies. -
Anti-inflammatory Agent
NLRP3-IN-72 is a benzimidazole derivative that functions as an anti-inflammatory agent by specifically targeting the NLRP3 inflammasome. It demonstrates significant biological activity with an IC50 of 0.3 μM for inhibiting NLRP3-mediated IL-1β secretion, a PD50 of 0.4 μM for protecting against pyroptosis, and an EC50 of 0.6 μM for the induction of heme oxygenase-1 (HO-1). These properties make NLRP3-IN-72 a valuable tool for research into inflammatory processes and potential therapeutic interventions. -
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. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-4 is a potent dual-target inhibitor of CYP51 and PD-L1, demonstrating IC50 values of 0.17 μM and 0.021 μM, respectively. This compound exhibits significant antifungal activity and is effective against drug-resistant fungal strains in vitro. CYP51/PD-L1-IN-4 is suitable for research applications focused on fungal infections and the interplay between fungal pathogens and immune checkpoint regulation. -
Anti-Inflammatory Agent; LXRα Activator
Taraxasterol is a pentacyclic triterpenoid that acts as an LXRα activator, demonstrating significant anti-inflammatory properties. Isolated from Taraxacum mongolicum, this compound has potential applications in the study of immune-inflammatory diseases, contributing to our understanding of metabolic regulation and inflammatory pathways. Researchers exploring therapeutic strategies for inflammatory conditions may find Taraxasterol an invaluable tool for investigation. -
Drug Metabolite
3-O-Methyldopa is a metabolite of L-DOPA that can effectively cross the blood-brain barrier. This compound has been shown to inhibit the astrocyte-mediated protective effects of L-DOPA on dopaminergic neurons, offering insights into its role in neurobiology. Additionally, 3-O-Methyldopa exhibits antidepressant and neuroprotective properties, making it a valuable tool for research into nervous system disorders, including depression and Parkinson's disease. -
HIFU Enhancer
Perfluorohexane functions as a HIFU (high-intensity focused ultrasound) enhancer, improving the efficacy and precision of ultrasound therapies while minimizing collateral damage to surrounding tissues. This perfluorocarbon compound has been shown to elevate the levels of heme oxygenase-1 (HO-1) and interleukin-10 (IL-10), thereby exhibiting antioxidant properties. Additionally, perfluorohexane plays a significant role in mitigating lung injury induced by lipopolysaccharide (LPS), making it a valuable tool for research into acute lung injury and related therapeutic applications. -
Endogenous Metabolite
5-Methoxy-DL-tryptophan is an endogenous metabolite that exhibits anti-inflammatory properties. This compound is known to inhibit lipopolysaccharide-induced release of interleukin-6 (IL-6), thereby suggesting its role in inflammatory processes. Its biological activity makes it a valuable tool for research in the context of atherosclerosis and related inflammatory conditions. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
PDE4 Inhibitor
Morcamilast is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, exhibiting IC50 values of 1.28 nM for PDE4A1A, 2.33 nM for PDE4B1, and 1.63 nM for PDE4D2. This compound demonstrates significant anti-inflammatory activity by inhibiting the lipopolysaccharide (LPS)-induced release of pro-inflammatory cytokines, including TNF-α, IL-12/23p40, IL-23, and IL-17A in human peripheral blood mononuclear cells (PBMCs) and T cells. Morcamilast also exhibits antipruritic effects, making it a valuable tool for investigating psoriasis, atopic dermatitis, and various other inflammatory disorders. -
PDE1C Inhibitor
PDE1-IN-9 is a selective inhibitor of phosphodiesterase 1 (PDE1), demonstrating an IC50 of 11 nM for PDE1C. This compound significantly reduces the mRNA expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α, as well as iNOS, while inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 also showcases favorable metabolic stability in rat liver microsomes, making it a valuable tool for studying PDE1-related pathways and inflammatory responses. -
PDE4 Inhibitor
Mesopram is a selective phosphodiesterase (PDE) 4 inhibitor that effectively reduces the synthesis of pro-inflammatory cytokines, including TNF-α and IFN-γ. This compound has shown efficacy in alleviating Dextran sulfate sodium (DSS)-induced colitis in murine models, making it a valuable tool for research in chronic inflammatory diseases. Mesopram can be employed to investigate therapeutic strategies aimed at modulating inflammatory responses. -
PPARγ Modulator
GED 0507-34-Levo is an orally active modulator of PPARγ. This compound effectively downregulates the expression of TGF-β, Smad3, IL-13, and CTGF in colon tissue. GED 0507-34-Levo has demonstrated therapeutic potential in improving symptoms of DSS-induced chronic colitis and associated fibrosis, making it a valuable tool for research in inflammatory bowel diseases and fibrotic disorders. -
AhR Modulator
AhR Modulator-1 (6-MCDF) is a selective and orally active modulator of the aryl hydrocarbon receptor (AhR). This compound demonstrates significant inhibition of metastasis by reducing vascular endothelial growth factor (VEGF) production in prostatic tissues prior to tumor formation. Additionally, AhR Modulator-1 exhibits anti-estrogenic effects in the rat uterus, making it a valuable tool for investigating the roles of AhR in cancer biology and endocrine regulation. -
Drug Metabolite
Regorafénib N-oxyde (M2) is an active metabolite of Regorafenib, functioning as a multi-target inhibitor. It effectively targets VEGFR1/2/3, PDGFRβ, Kit, RET, and Raf-1, exhibiting IC50 values of 13, 4.2, 46, 22, 7, 1.5, and 2.5 nM, respectively. This compound is essential for studies involving cancer research and drug metabolism, providing insights into the pharmacological effects and therapeutic potential of Regorafenib. -
MAO-A/DYRK1A Inhibitor
Norharmine is a Harmine analogue that functions as an inhibitor of monoamine oxidase A (MAO-A) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A). It exhibits weak inhibitory activity against MAO-A and demonstrates certain inhibitory effects on DYRK1A, positioning it as a valuable tool for research in neurobiology and cellular signaling pathways. Norharmine is useful in studies focusing on mood disorders and cognitive functions related to these kinase targets. -
Endogenous Metabolite
Ethyl glucuronide is an endogenous metabolite of ethanol, serving as a reliable biomarker for alcohol exposure. It accumulates in hair, providing a measure of alcohol intake over extended periods. Additionally, ethyl glucuronide acts as an agonist for Toll-like receptor 4 (TLR4), making it relevant in studies of inflammatory responses and alcohol metabolism. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride is a potent inhibitor of phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4), and phosphodiesterase 5 (PDE5), with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. Additionally, it acts as an antagonist of the H1-histamine receptor, contributing to its anti-inflammatory properties. Fenspiride is primarily utilized in research related to respiratory diseases, offering insights into mechanisms of action and potential therapeutic applications. -
5-Lipoxygenase Inhibitor
Linetastine is a potent, orally active inhibitor of 5-Lipoxygenase, an enzyme critical in the synthesis of leukotrienes. By inhibiting this pathway, Linetastine demonstrates significant antihistamine activity, effectively reducing leukotriene B4 and C4 release from calcium ionophore-stimulated human leukocytes. This compound is particularly useful in research applications focused on inflammatory processes and allergic responses, providing insights into the modulation of leukotriene-mediated pathways. -
HSP70 Ligand
HSP70 Ligand 1 serves as a ligand for the heat shock protein 70 (HSP70), facilitating the development of PROTAC molecules. This compound is instrumental in synthesizing PROTAC HSP70 Degrader-1, enabling targeted protein degradation studies. It is valuable for researchers investigating HSP70's role in cellular stress responses and therapeutic applications. -
Endogenous Metabolite
Palmitic acid sodium is a long-chain saturated fatty acid that serves as an endogenous metabolite. It has been shown to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in mouse granulosa cells. This compound is commonly utilized to establish a cell steatosis model, making it valuable for research into metabolic disorders and related cellular mechanisms. -
Combined with Hsp90
AMP-PCP disodium is an ATP analogue that specifically targets the N-terminal domain of Hsp90, exhibiting a dissociation constant (Kd) of 3.8 μM. By binding to Hsp90, AMP-PCP disodium promotes the formation of its active homodimer, facilitating studies on protein folding and maturation. This reagent is valuable for research applications focusing on molecular chaperones and their roles in cellular stress responses. -
HSP Inhibitor
Apatorsen sodium is a 2'-methoxyethyl-modified antisense oligonucleotide targeting Hsp27. It effectively reduces Hsp27 mRNA and protein levels, disrupting stress-induced cytoprotective functions, promoting apoptosis, inhibiting tumor growth, and preventing metastasis. This compound is relevant for research applications in non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, and bladder cancer. -
Hsp90-Cdc37 PPI Inhibitor
DDO-5936 is a potent inhibitor of the Hsp90-Cdc37 protein-protein interaction. This compound specifically disrupts the chaperone-client complex, leading to altered protein folding and degradation pathways. Its biological activity makes DDO-5936 a valuable tool for research applications focused on colorectal cancer and other related therapeutic areas. -
HSPA5 Inhibitor
HM03 is a selective inhibitor of HSPA5 (Heat Shock Protein 70kDa, also known as Bip or Grp78). This compound exhibits significant anticancer activity, making it a valuable tool for cancer research. It can be utilized to study the role of HSPA5 in tumor progression and therapeutic resistance, providing insights into potential treatment strategies targeting this chaperone protein. -
HSP Co-Inducer
Arimoclomol is an orally active co-inducer of heat shock proteins (HSP). It functions by enhancing Hsp expression, thereby providing protection to motor neurons through the modulation of protein aggregation and promoting the clearance of misfolded proteins via the proteasome-ubiquitin system. This compound is particularly relevant for research applications concerning Niemann-Pick disease type C, as it effectively crosses the blood-brain barrier, facilitating its therapeutic potential in neurological disorders. -
Hsp90 Inhibitor
Zelavespib hydrochloride is a potent inhibitor of the heat shock protein 90 (Hsp90), exhibiting an IC50 of 51 nM in MDA-MB-468 cancer cell lines. This compound disrupts Hsp90 function, leading to the degradation of client oncoproteins, thereby demonstrating significant potential in cancer research. Zelavespib is utilized in studies focused on the therapeutic targeting of Hsp90 for various malignancies. -
HSP Co-Inducer
Arimoclomol citrate is an orally active co-inducer of heat shock proteins (HSPs). It enhances the expression of HSPs, thereby protecting motor neurons by facilitating the clearance of misfolded proteins via the proteasome-ubiquitin system. This compound is particularly relevant for research applications concerning Niemann–Pick disease type C and studies of neurodegenerative disorders linked to protein aggregation. -
Hsp70 Inhibitor
YM-1 is an orally active inhibitor of the heat shock protein 70 (Hsp70). This compound has been shown to induce apoptosis in HeLa cells while also up-regulating key regulatory proteins such as p53 and p21. Its effects on cell viability and protein expression make YM-1 a valuable tool for studying the role of Hsp70 in cancer biology and therapeutic applications.
