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Catalog No.
Product Name
Application
Product Information
Citations
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Protease Inhibitor
Patamostat hydrochloride is a highly effective protease inhibitor, targeting trypsin, plasmin, and thrombin with IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively. It demonstrates potential in suppressing the pathogenesis and progression of acute pancreatitis, making it a valuable tool for research focused on protease-related diseases and therapeutic interventions. -
Tyrosinase Inhibitor
Cepharadione B is a natural tyrosinase inhibitor derived from the leaves of Piper sanctum, exhibiting an IC50 value of 170 μM. This compound demonstrates significant inhibitory effects on cell growth in various cancer cell lines, including A-549, SK-OV-3, SK-MEL-2, XF-498, and HCT-15. Cepharadione B is valuable for research exploring pigmentation processes, melanoma, and potential therapeutic interventions against cancer. -
Thrombin/ Factor Xa Inhibitor
Ciraparantag is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants. This compound effectively neutralizes the effects of low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. Its unique mechanism makes Ciraparantag a valuable tool for research focused on anticoagulation reversal and hemostasis. -
Thrombin/Factor Xa Inhibitor
Ciraparantag acetate is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants, including low molecular weight heparins, unfractionated heparins, and certain direct oral anticoagulants, excluding vitamin K antagonists (VKAs). Its primary mechanism targets the coagulation pathway, facilitating the restoration of normal hemostasis in clinical situations where anticoagulation reversal is necessary. Ciraparantag acetate is valuable in research applications focused on anticoagulation management and hemostatic balance in cardiovascular studies. -
Thrombin Inhibitor
Edoxaban impurity 4 is a structural impurity related to Edoxaban, a selective and potent thrombin inhibitor. It demonstrates significant biological activity and is primarily utilized in research applications focusing on anticoagulation strategies. Edoxaban itself serves as an effective anticoagulant, with its mechanistic role in inhibiting factor Xa contributing to therapeutic approaches for stroke prevention and other thromboembolic disorders. -
Thrombin/Factor Xa Inhibitor
Ciraparantag TFA is a potent thrombin and factor Xa inhibitor utilized as a broad-spectrum reversal agent for anticoagulants. It effectively antagonizes the effects of various anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and specific direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. This compound is significant for research applications focused on enhancing hemostatic management in patients receiving anticoagulant therapy. -
Thrombin/Factor Xa/Trypsin/Papain Inhibitor
Bacithrocin D is a potent inhibitor of key proteases, specifically targeting thrombin, factor Xa, trypsin, and papain. It effectively prolongs clotting time, making it valuable in studies related to coagulation and hemostasis. Bacithrocin D demonstrates IC50 values of 124 μM for thrombin, 9 μM for factor Xa, 0.85 μM for trypsin, and a remarkable 0.01 μM for papain, showcasing its high potency against these proteases. This reagent is useful for investigating protease-related pathways and developing therapeutic strategies in anticoagulation research. -
Thrombin Inhibitor
Bacithrocin A is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain, demonstrating IC50 values of 48 μM, 13 μM, 0.65 μM, and 0.02 μM, respectively. This compound is of particular interest in the study of coagulation processes and the development of anticoagulant therapies. Its broad-spectrum inhibitory activity makes it a valuable reagent for biological research focused on protease activity modulation and hemostasis. -
Thrombin Inhibitor
Bacithrocin C is a potent thrombin inhibitor that effectively targets thrombin, factor Xa, trypsin, and papain, exhibiting IC50 values of 80 μM, 15 μM, 1.3 μM, and 0.02 μM, respectively. This compound demonstrates significant inhibitory activity, making it a valuable tool for research in coagulation pathways and protease-related studies. It is suitable for applications focused on understanding thrombotic processes and developing antithrombotic strategies. -
Thrombin Inhibitor
Bacithrocin B is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain. It exhibits inhibitory activity with IC50 values of 84 μM for thrombin, 17 μM for factor Xa, 1.7 μM for trypsin, and 0.02 μM for papain. This compound is valuable for research applications aiming to study coagulation processes and enzyme dynamics in various biological systems. -
Calpain Inhibitor
Calpain Inhibitor V (Mu-Val-HPh-FMK) is an irreversible inhibitor of calpain, designed for effective cellular penetration. This compound exhibits notable anti-chlamydial activity and is utilized in research exploring calpain-mediated pathways and their implications in various diseases. Its application extends to studies focused on cellular signaling processes and the therapeutic potential of calpain modulation. -
AT1/NEP Inhibitor
TD-0212 TFA is an orally active dual pharmacology inhibitor targeting the angiotensin II type 1 receptor (AT1) and neprilysin (NEP). With a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP, this compound exhibits significant biological activity in modulating cardiovascular and neuroprotective pathways. TD-0212 TFA is suitable for research applications exploring the roles of AT1 antagonism and neprilysin inhibition in various disease models. -
Cell-penetrating Peptide/Proteasome Inhibitor
Octaarginine is a cell-penetrating peptide and potent proteasome inhibitor. It exhibits mixed-type inhibition against the chymotrypsin-like, caspase-like, and trypsin-like activities of the 20S proteasome while displaying reduced efficacy against the 26S proteasome. This compound facilitates the accumulation of ubiquitin-conjugated proteins and promotes HSPG-dependent cellular internalization through macropinocytosis, thereby enhancing the uptake of liposomal cargo and gene delivery. Octaarginine is valuable for research related to cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections. -
Aminopeptidase B Inhibitor
Arphamenine B hemisulfate is a selective inhibitor of aminopeptidase B, a Zn2+-dependent exopeptidase that primarily cleaves arginine and lysine residues from the N-terminus of peptide substrates. This compound is derived from bacterial sources and has been shown to enhance immune responses. Arphamenine B hemisulfate is utilized in research for characterizing novel proteases and investigating their biological roles. -
Proteasome Inhibitor
PR-39 is a natural proline- and arginine-rich antibacterial peptide that functions as a noncompetitive, reversible allosteric inhibitor of the proteasome. By binding to the α7 subunit of the proteasome, PR-39 effectively blocks the degradation of NF-κB inhibitor IκBα through the ubiquitin-proteasome pathway. This compound demonstrates key biological activities such as stimulating angiogenesis and inhibiting inflammatory responses, making it a valuable tool for research on myocardial infarction and inflammatory diseases. -
NEP/APN Inhibitor
Sialorphin targets neprilysin (NEP) and aminopeptidase N (APN) as a potent inhibitor, effectively preventing the degradation of key neuropeptides like Substance P and methionine enkephalin. This compound demonstrates significant biological activity, including analgesic effects, modulation of sexual behavior in male rats, and the alleviation of colitis. Additionally, Sialorphin exhibits low toxicity against specific tumor cells, making it a valuable tool for research into pain management, inflammatory bowel disease, and oncology. -
Proteasome Inhibitor
Antitrypanosomal agent 15 is a selective proteasome inhibitor targeting Trypanosoma cruzi, with an impressive pIC50 of 7.4 for the T. cruzi proteasome and minimal activity (pIC50 < 4) against human proteasomes. This orally active compound demonstrates excellent brain penetration and favorable ADME properties, making it suitable for research focused on Chagas disease and related therapeutic interventions. Its selectivity and efficacy highlight its potential for advancing studies in trypanosomiasis. -
PfDHODH Inhibitor
PfDHODH-IN-3 is a potent inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 47 nM. This compound exhibits strong antimalarial activity, effectively inhibiting the growth of Plasmodium in animal models. PfDHODH-IN-3 is valuable for research focused on antimalarial drug development and understanding the mechanisms of Plasmodium resistance. -
20S Proteasome Inhibitor
20S Proteasome-IN-4 is a selective inhibitor of the 20S proteasome, exhibiting an IC50 of 6.3 nM against Trypanosoma brucei brucei. This brain-penetrant compound is orally active and demonstrates potential for research into human African trypanosomiasis (HAT). Its specificity for the parasite makes it a valuable tool for studying proteasomal functions in this significant infectious disease. -
Proteasome Inhibitor
LXE408 fumarate is a non-competitive proteasome inhibitor selectively targeting kinetoplastids. It exhibits potent inhibitory activity with an IC50 of 0.04 μM against the L. donovani proteasome, demonstrating an EC50 of 0.04 μM for L. donovani itself. With limited ability to penetrate the blood-brain barrier, LXE408 fumarate is primarily suitable for research in visceral leishmaniasis (VL). -
Proteasome Inhibitor
Carmaphycin-17 is a selective 20S proteasome inhibitor, with an EC50 value of 217 nM. This compound exhibits strong antimicrobial activity against Trichomonas vaginalis, effectively overcoming Metronidazole resistance. It significantly reduces parasite burden in a topical treatment model without noted adverse effects. Carmaphycin-17 is a valuable tool for research on sexually transmitted diseases, specifically trichomoniasis. -
PfDHODH Inhibitor
DSM267 is a triazolopyrimidine compound that preferentially inhibits Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 38 nM, demonstrating significant selectivity over human DHODH with an IC50 exceeding 100,000 nM. This reagent is valuable for in vitro systematic screening and characterizing the pathways of resistance evolution in Plasmodium falciparum against DHODH inhibitors. Its use supports research into antimalarial resistance mechanisms and facilitates the development of novel therapeutic strategies. -
Pf Proteasome Inhibitor
Proteasome-IN-8 is a specific inhibitor of the proteasome in Plasmodium falciparum. This compound demonstrates notable antiparasitic activity against the P. falciparum 3D7 strain. It is a valuable tool for research into the mechanisms of malaria pathogenesis and the development of therapeutic strategies targeting parasitic proteasomes. -
DHODH Inhibitor
Genz-669178 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), demonstrating an IC50 range of 0.015-0.05 μM against Plasmodium species. It effectively inhibits P. berghei and P. falciparum strains 3D7 and Dd2, with respective IC50 values of 0.068, 0.008, and 0.01 μM. In vivo studies indicate that Genz-669178 exhibits significant anti-malarial efficacy in P. berghei-infected mice, with an ED50 of 13-21 mg/kg/day, alongside favorable pharmacokinetic properties. This compound serves as a valuable tool for malaria research and drug development. -
PfDHODH/PbDHODH Inhibitor
DSM74 is a potent inhibitor of dihydroorate dehydrogenase (DHODH) in both Plasmodium falciparum (PfDHODH) and Plasmodium berghei (PbDHODH), with IC50 values of 0.28 μM and 0.38 μM, respectively. This orally active compound exhibits significant antimalarial activity, effectively inhibiting the growth of Plasmodium species in animal models. It is a valuable tool for researchers investigating the mechanisms of malaria and developing novel therapeutic strategies. -
PfDHODH Inhibitor
BRD7539 is a potent inhibitor of PfDHODH, exhibiting an IC50 value of 0.033 μM. This compound demonstrates significant efficacy against multidrug-resistant asexual blood-stage Plasmodium falciparum (Dd2 strain) with an EC50 of 0.010 μM, as well as against liver-stage Plasmodium berghei, with an EC50 of 0.015 μM. BRD7539 serves as a valuable tool for research targeting malaria drug development and resistance mechanisms. -
Aminopeptidase B Inhibitor
Arphamenine B is a selective inhibitor of aminopeptidase B, a Zn2+-dependent exopeptidase that cleaves arginine and lysine residues from the amino terminus of peptide substrates. This compound enhances immune responses and serves as a valuable tool for the characterization of novel proteases in biochemical research. Its unique mechanism provides insights into protein metabolism and potential therapeutic applications. -
RORγ/DHODH Inhibitor
Izumerogant (IMU-935) is an orally active dual inhibitor of RORγ and DHODH, with IC50 values of 10 nM and 98 nM, respectively. This compound effectively disrupts the replication of various viruses, including SARS-CoV-2, HCMV, and HAdV5, demonstrated by EC50 values ranging from 3.6 to 17 nM. Izumerogant serves as a valuable tool for investigating antiviral mechanisms and therapeutic strategies against viral infections. -
NS2B-NS3/thrombin Inhibitor
5-((1H-Indol-3-yl)methylene)imidazolidine-2,4-dione is a potent inhibitor of the dengue virus NS2B-NS3 protease and thrombin. This compound is valuable for studying the mechanisms of viral replication and coagulation processes, making it an essential tool in research focused on infectious diseases and related therapeutic interventions. Its dual activity highlights its potential for investigating the dynamics of viral pathology and thrombotic complications. -
MMP/TACE/ADAM Inhibitor
(R)-TAPI-2 is a potent inhibitor targeting matrix metalloproteinases (MMPs), tumor necrosis factor alpha-converting enzyme (TACE), and a disintegrin and metalloproteinase (ADAM), exhibiting an IC50 value of 20 μM for MMP activity. This compound is utilized in research focused on inflammation, cancer progression, and cell signaling due to its ability to modulate proteolytic processes. Additionally, (R)-TAPI-2 has demonstrated efficacy in preventing viral entry, specifically in the context of SARS-CoV infections, making it valuable for virology studies. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-2 is a potent dual inhibitor of RORγ and DHODH, exhibiting IC50 values of 11.9 nM and 90 nM, respectively. This compound demonstrates significant antiviral activity against multiple viruses, including SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively. RORγ/DHODH-IN-2 is ideal for research applications targeting immune signaling pathways and viral infections. -
Aminopeptidase N/Leukotriene A4 Hydrolase Inhibitor
Bestatin trifluoroacetate is a potent inhibitor of CD13 (Aminopeptidase N) and leukotriene A4 hydrolase. It plays a significant role in cancer research by modulating enzymatic activity associated with tumor progression and inflammation. With its capability to interfere with amino acid metabolism, Bestatin trifluoroacetate is valuable for studying the biological processes linked to these targets. -
Aminopeptidase N/Leukotriene A4 Hydrolase Inhibitor
Bestatin hydrochloride is an inhibitor of aminopeptidase N (CD13) and leukotriene A4 hydrolase. It plays a significant role in cancer research by modulating the enzymatic activities associated with tumor progression and inflammatory processes. This compound is valuable for studies investigating the implications of aminopeptidases in tumor microenvironments and immune responses. -
Tyrosinase Inhibitor
2-Hydroxy-4-methoxybenzaldehyde is a potent inhibitor of the enzyme tyrosinase, which is crucial in melanin biosynthesis. This compound plays a significant role in research pertaining to pigmentation disorders and skin-related applications. Additionally, it can be utilized as a precursor for the synthesis of Urolithin M7, expanding its utility in biochemical studies. -
Aminopeptidase Inhibitor
Amastatin hydrochloride is a potent competitive inhibitor of aminopeptidases, exhibiting slow, tight binding kinetics. It demonstrates Ki values of 0.26 nM, 30 nM, and 52 nM against Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, and microsomal aminopeptidase, respectively. This compound is valuable for research applications focusing on protein metabolism and post-translational modifications, as well as in studies exploring the role of aminopeptidases in various physiological and pathological processes. -
Immunoproteasome Inhibitor
Argyrin B is a natural cyclic peptide that functions as a reversible, non-competitive inhibitor of the immunoproteasome. It demonstrates selective inhibition of the β5i and β1i subunits, with a nearly 20-fold preference for β1i over the corresponding β1c subunit found in the constitutive proteasome. In addition to its role in proteasome inhibition, Argyrin B exhibits significant antibacterial properties, making it valuable for research in immunology and antimicrobial studies. -
DHODH Inhibitor
DHODH-IN-17 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), with an IC50 value of 0.40 μM. This compound is pivotal for studying the metabolic pathways involved in acute myeloid leukemia (AML) and may aid in the development of targeted therapies for this condition. Its ability to inhibit DHODH highlights its potential use in cancer research, particularly in understanding tumor metabolism and proliferation. -
DHODH Inhibitor
DHODH-IN-23 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), a key enzyme in the de novo pyrimidine synthesis pathway. This compound exhibits significant biological activity in cancer research, facilitating the exploration of metabolic pathways and their implications in tumorigenesis. DHODH-IN-23 serves as a valuable tool for studies aiming to elucidate the role of pyrimidine metabolism in cancer cell proliferation and survival. -
hDHODH Inhibitor
hDHODH-IN-13 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH), with an IC50 value of 173.4 nM. This compound demonstrates significant potential in the investigation of inflammatory bowel disease (IBD) by modulating pyrimidine biosynthesis. hDHODH-IN-13 is a valuable tool for exploring therapeutic strategies targeting hDHODH in various disease models. -
DHODH Inhibitor
(E/Z)-Ginkgolic acid C17:2 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), a key enzyme in the de novo pyrimidine biosynthesis pathway. This compound, derived from Ginkgo biloba, demonstrates the ability to bind tightly to the target enzyme, mediating its biological activity. Its inhibitory effect on DHODH makes it a valuable reagent for studying cellular proliferation, autoimmune diseases, and potential anti-cancer strategies. -
hDHODH Inhibitor
hDHODH-IN-8 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibiting an IC50 value of 16 nM. This compound demonstrates significant antiproliferative effects and possesses excellent solubility in aqueous solutions. hDHODH-IN-8 is particularly relevant for research exploring tumorigenesis, with potential implications in lymphoma studies. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-1 is a dual inhibitor targeting retinoic acid receptor-related orphan receptor gamma t (RORγt) and dihydroorotate dehydrogenase (DHODH). With IC50 values of 0.083 μM for RORγt and 0.172 μM for DHODH, this compound demonstrates significant potency. RORγt/DHODH-IN-1 has been shown to possess notable in vivo anti-inflammatory activity, making it a valuable tool for research in immunology and inflammation-related studies. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-3 is a dual inhibitor targeting both RORγt and dihydroorotate dehydrogenase (DHODH), exhibiting IC50 values of 0.098 μM for RORγt and 0.432 μM for DHODH. This compound demonstrates significant in vivo anti-inflammatory activity, making it a valuable tool for researchers investigating autoimmune diseases and other inflammatory conditions. Its dual mechanism of action positions it as a promising candidate for therapeutic development in these areas. -
hDHODH Inhibitor
hDHODH-IN-11 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibiting an IC50 value of 7.2 nM. This compound demonstrates low cytotoxicity, making it suitable for in vitro studies. hDHODH-IN-11 is primarily utilized in research focused on acute myeloid leukemia (AML), contributing to the understanding of therapeutic targets within this malignancy. -
hDHODH Inhibitor
hDHODH-IN-10 is a selective and potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), demonstrating an IC50 value of 10.9 nM. This compound exerts its biological activity through hydrogen bonding interactions with key residues, including Arg136 and Gln47. hDHODH-IN-10 effectively inhibits the proliferation of cancer cells and is useful for research applications related to various malignancies, such as acute myeloid leukemia (AML) and colorectal cancer. -
RORγt/DHODH Inhibitor
RORγt/DHODH-IN-2 is a potent dual inhibitor of RORγt and DHODH, targeting key pathways involved in immune regulation and inflammation. This compound exhibits significant biological activity that can be leveraged in the investigation of inflammatory bowel disease (IBD) and related immune disorders. Its dual action provides a valuable tool for research into therapeutic strategies aimed at modulating RORγt and DHODH activity in inflammatory contexts. -
DHODH Inhibitor
DHODH-IN-18 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), with an IC50 value of 0.2 nM. This compound effectively modulates the de novo pyrimidine biosynthesis pathway, making it a valuable tool in studies of cell proliferation and differentiation. DHODH-IN-18 is suitable for research applications in cancer biology and autoimmune disorders, where DHODH plays a critical role. -
DHODH Inhibitor
DHODH-IN-21 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor, exhibiting an IC50 value of 1.1 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for research into acute myeloid leukemia (AML). Its high potency and specificity for DHODH facilitate investigations into the mechanistic roles of this enzyme in cancer biology. -
DHODH Inhibitor
DHODH-IN-22 is a highly selective and orally bioavailable inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 0.3 nM. This compound demonstrates significant potential in the research of acute myelogenous leukemia (AML) by modulating pyrimidine synthesis and impacting cell proliferation. Its properties make DHODH-IN-22 a valuable tool for studying the biochemical pathways involved in AML and evaluating novel therapeutic strategies. -
DHODH Inhibitor
Indoluidin E is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), an enzyme involved in the de novo pyrimidine biosynthesis pathway. This compound has demonstrated notable inhibitory effects on cancer cell proliferation, making it a valuable tool for cancer research. Its mechanistic action allows for potential applications in studying metabolic pathways and developing therapeutic strategies targeting DHODH in various malignancies.
