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Catalog No.
Product Name
Application
Product Information
Citations
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TrxR Inhibitor
TrxR-IN-6 is an inhibitor of thioredoxin reductase (TrxR), a key enzyme in maintaining the cellular redox balance. This compound induces the accumulation of reactive oxygen species (ROS), leading to mitochondrial dysfunction, endoplasmic reticulum (ER) stress, and DNA damage. TrxR-IN-6 effectively promotes oxidative stress, resulting in apoptosis, making it a valuable tool for cancer research and studies focusing on oxidative stress mechanisms. -
PARP1/NAMPT Inhibitor
PARP1/NAMPT-IN-1 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 1.2 nM and 6.7 nM, respectively. This compound disrupts the homologous recombination repair pathway, leading to the accumulation of DNA double-strand breaks, which induces cell cycle arrest and apoptosis. Additionally, PARP1/NAMPT-IN-1 demonstrates antimigratory effects and has shown significant antitumor activity in a breast cancer xenograft model. It is a valuable tool for research on triple-negative breast cancer (TNBC). -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
PfHsp90 Inhibitor
Ursolic acid acetate is a triterpenoid compound that inhibits Plasmodium falciparum heat shock protein 90 (PfHsp90) with a binding affinity (KD) of 8.16 μM. It exhibits cytotoxic effects on KB cells, with an IC50 value of 8.4 μM. This compound is suitable for applications in tumor research and antimalarial studies, providing a valuable tool for investigating the role of heat shock proteins in disease mechanisms. -
HSP70 Allosteric Inhibitor
MAL3-101 is a potent allosteric inhibitor of the heat shock protein 70 (HSP70), primarily acting by inhibiting the ATPase activity of HSP70 through disruption of the Hsp40 co-chaperone interaction. This compound has demonstrated significant biological activity in cellular models, making it a valuable tool for investigating the role of HSP70 in muscle invasive bladder cancer (MIBC) research. Researchers can utilize MAL3-101 to explore therapeutic strategies targeting this molecular chaperone in cancer treatment. -
HSP90 Inhibitor
Icapamespib hydrochloride is a selective inhibitor of HSP90, targeting epichaperome assembly with slow dissociation kinetics. This compound effectively disrupts disease-related protein interaction networks, reducing neurotoxic protein aggregation and hindering tumor cell survival signals. Icapamespib hydrochloride is valuable in research focused on neurodegenerative diseases, including Alzheimer's disease, along with various cancers, such as glioblastoma and metastatic breast cancer. -
HSP90 Inhibitor
Icapamespib is a selective inhibitor of HSP90 that effectively disrupts epichaperome formation through non-covalent binding, exhibiting slow dissociation kinetics. This compound is capable of crossing the blood-brain barrier, facilitating the disassembly of abnormal protein interaction networks and reducing neurotoxic protein aggregation. Icapamespib demonstrates potential in research applications focused on neurodegenerative diseases, including Alzheimer’s disease, as well as various cancers such as glioblastoma and metastatic breast cancer. -
Hsp90 Inhibitor
SNX-0723 is a potent Hsp90 inhibitor that exhibits anti-Plasmodium activity. It demonstrates notable binding affinity for human Hsp90 and Plasmodium falciparum Hsp90, with inhibition constants (Kis) of 4.4 nM and 47 nM, respectively. Additionally, SNX-0723 effectively inhibits liver-stage Plasmodium berghei ANKA parasites, with an EC50 value of 3.3 μM, making it a valuable tool for research into malaria treatment and Hsp90-related biological processes. -
HSP70 ATPase Inhibitor
Displurigen (NSC375009) is an HSP70 ATPase inhibitor that specifically targets HSPA8, disrupting the pluripotency of human embryonic stem cells. This compound effectively inhibits the ATPase activity of HSP70 with an IC50 of 225 μM, making it a valuable tool for research in stem cell biology and differentiation processes. Its mechanism of action provides insights into cellular signaling pathways related to stem cell maintenance and development. -
HSP90β Inhibitor
KUNB31 is a selective inhibitor of HSP90β, exhibiting a binding affinity with a Kd value of 0.18 μM. This compound disrupts the function of the HSP90β protein, which is implicated in the maturation and stabilization of client proteins involved in cancer and other diseases. KUNB31 is valuable for research focused on cellular stress responses, protein homeostasis, and therapeutic strategies targeting protein chaperones. -
Hsp90 Inhibitor
Hsp90-IN-37 is a potent inhibitor of heat shock protein 90 (Hsp90), demonstrating a 69% reduction in enzymatic activity. This compound exhibits significant antitumor properties, making it a valuable tool in cancer research. Hsp90-IN-37 can be utilized to explore the role of Hsp90 in cancer cell survival and proliferation, supporting efforts to develop targeted therapies. -
Hsp90 Inhibitor
3-Phenyltoxoflavin is an Hsp90 inhibitor that interacts with the Hsp90-TPR2A complex, exhibiting a dissociation constant (Kd) of 585 nM. This compound demonstrates significant anti-cancer properties, making it a valuable tool for cancer research. Its ability to inhibit Hsp90 function provides insights into the molecular mechanisms of cancer cell growth and survival, supporting studies aimed at developing targeted therapies. -
HSP90 Inhibitor
Hsp90-IN-17 hydrochloride is a potent inhibitor of Heat Shock Protein 90 (HSP90), a chaperone protein involved in protein folding and stabilization. This compound demonstrates significant biological activity by disrupting the chaperoning function of HSP90, leading to the degradation of oncogenic client proteins. Hsp90-IN-17 is primarily used in research applications focused on proliferative diseases, including various cancer types and neurodegenerative disorders, providing insights into therapeutic strategies targeting HSP90. -
HSP90 Inhibitor
HSP90-IN-23 is a potent inhibitor of heat shock protein 90 (HSP90) with an IC50 value of 9 nM. This compound effectively induces apoptosis in tumor cells and successfully arrests the cell cycle in the G0/G1 phase. HSP90-IN-23 is an invaluable tool for cancer research, facilitating the study of HSP90's role in tumorigenesis and potential therapeutic strategies. -
HSP70 Inhibitor
AP-4-139B is a potent inhibitor of HSP70, exhibiting an IC50 of 180 nM against human HSP70. Its mechanism involves direct binding to HSP70, leading to the inhibition of ATPase activity. By facilitating the phosphorylation of Beclin-1, AP-4-139B promotes autophagy. This compound has demonstrated significant antitumor activity in preclinical models of colorectal cancer and pancreatic ductal adenocarcinoma, making it a valuable tool for cancer research. -
Hsp90 Inhibitor
HSP90-IN-22 is an inhibitor of heat shock protein 90 (Hsp90) that exhibits significant antiproliferative activity in cancer cells. The compound demonstrates IC50 values of 3.65 μM in MCF7 breast cancer cells and 2.71 μM in SKBr3 breast cancer cells. This compound is valuable for research into cancer cell biology and the therapeutic potential of Hsp90 inhibition in cancer treatment.
