Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
Nek1 Inhibitor
BSc5367 is a potent inhibitor of NIMA-related protein kinase 1 (Nek1), exhibiting an IC50 of 11.5 nM. Nek1 is integral to cell cycle regulation, DNA repair, and microtubule dynamics, with its dysfunction implicated in various conditions such as amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD), and radiotherapy-resistant cancers. This reagent is valuable for research into the molecular mechanisms underlying these diseases and for exploring potential therapeutic interventions. -
Nek7 Inhibitor
Ofirnoflastum is a selective inhibitor of the serine/threonine-protein kinase Nek7. This compound demonstrates significant anti-inflammatory properties, making it a valuable tool for research into inflammation-related pathways and diseases. Its mechanism of action and specificity towards Nek7 facilitate investigations in various cellular processes, particularly those associated with cellular stress responses and mitotic regulation. -
NEK6 Inhibitor
ZINC05007751 is a selective inhibitor of the NIMA-related kinase NEK6, exhibiting an IC50 of 3.4 μM. This compound demonstrates notable antiproliferative effects across various human cancer cell lines and synergizes with Cisplatin and Paclitaxel in BRCA2-mutated ovarian cancer models. ZINC05007751 displays high specificity for NEK6 and NEK1, with minimal activity against NEK2, NEK7, and NEK9, making it a valuable tool for studying NEK6-related pathways in cancer research. -
Hec1/Nek2 Inhibitor
Nek2/Hec1-IN-3 is a potent inhibitor of the Hec1/Nek2 interaction, specifically designed to disrupt the binding between these two proteins. This compound exhibits significant biological activity by interfering with the Nek2-mediated regulation of cell division, making it a valuable tool for research in neoplastic diseases and cancer biology. Its application in studying tumorigenesis and cell cycle dysregulation facilitates a deeper understanding of oncogenic pathways. -
Nek2 Inhibitor
JH295 hydrate is a selective and irreversible inhibitor of NIMA-related kinase 2 (Nek2), exhibiting an IC50 value of 770 nM. This compound targets cellular Nek2 by inducing alkylation at Cys22, while showing no activity against critical mitotic kinases such as Cdk1, Aurora B, or Plk1, thereby maintaining bipolar spindle assembly and the spindle assembly checkpoint. Additionally, JH295 hydrate functions as a click chemistry reagent, possessing an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it valuable in various research applications. -
Nek2/Hec1 Inhibitor
Nek2/Hec1-IN-2 is a potent inhibitor of the Nek2 and Hec1 kinases. It effectively disrupts cell division processes, demonstrating inhibitory activity against cancer cell proliferation with an IC50 greater than 25 μM. This compound is valuable for research into mitotic regulation and therapeutic strategies targeting cancer cell growth. -
Nek2 Inhibitor
HCI-2184 is a potent Nek2 inhibitor with an IC50 value of 39.90 nM. This compound enhances the efficacy of Bortezomib by significantly inhibiting proteasome activity. HCI-2184 is valuable for research applications focused on cell cycle regulation and cancer therapeutics. -
Nek2 Inhibitor
Nek2-IN-6 is a selective inhibitor of never in mitosis (NIMA) related kinase 2 (Nek2), a critical regulator of mitotic processes. This compound demonstrates significant biological activity in inhibiting this kinase, making it valuable for exploring its role in cell division and related pathologies. Nek2-IN-6 is well-suited for research applications focused on cancer biology, particularly in studies examining the mitotic spindle assembly and its implications in tumorigenesis. -
NEK7 Inhibitor
NEK7-IN-1 is a potent inhibitor of NIMA-related kinase 7 (NEK7), exhibiting an IC50 of less than 100 nM. It effectively suppresses the release of IL-1β, with an IC50 of less than 50 nM. This compound is valuable for research into inflammatory responses and the molecular pathways involving NEK7. Its application extends to studies focused on cellular processes influenced by NEK7 modulation. -
Nek2 Inhibitor
Nek2-IN-5 is a potent and irreversible inhibitor of Nek2 (Never in mitosis gene a-related kinase 2). This compound features a clickable alkyne group, enabling it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-bearing molecules. Nek2-IN-5 is valuable in research applications focused on cell cycle regulation and cancer biology, providing insights into the role of Nek2 in cellular processes. -
Thrombin Receptor Activating Peptide
TRAP-7 is a thrombin receptor (PAR) activating peptide that functions by stimulating total inositol phosphate (IP) accumulation, as well as the phosphorylation of a specific endogenous substrate for activated protein kinase C (PKC). This compound is valuable in the study of signaling pathways related to thrombosis and cardiovascular diseases, providing insights into PAR-mediated cellular responses and potential therapeutic interventions. -
Thrombin Peptide
TP508 is a 23-amino acid nonproteolytic thrombin peptide that selectively targets the receptor-binding domain of thrombin. It activates endothelial nitric oxide synthase (eNOS) and promotes nitric oxide production in human endothelial cells, facilitating enhanced endothelial cell activation and stem cell recruitment. This molecule is of significant interest for applications in tissue revascularization and regenerative medicine research. -
MMP Inhibitor
Sucrose octasulfate is a matrix metalloproteinase (MMP) inhibitor that modulates cellular activities by regulating the extracellular matrix. It promotes the release of somatostatin-like immunoreactivity from gastric D cells, facilitating ulcer healing through increased endogenous somatostatin levels. This compound has demonstrated efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers, making it pertinent for research in chronic wound healing and gastrointestinal disorders. Additionally, sucrose octasulfate serves as a valuable pharmaceutical excipient in various therapeutic applications. -
MMP Inhibitor
Sucrose octasulfate sodium is a potent matrix metalloproteinase (MMP) inhibitor that enhances the release of somatostatin-like immunoreactivity (SLI) from gastric D cells. This compound promotes ulcer healing by increasing endogenous gastric somatostatin levels. Sucrose octasulfate sodium is utilized in research related to chronic wound healing and has shown significant efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers. Additionally, it serves as a useful pharmaceutical excipient in various applications. -
Microsomal Aminopeptidase
Microsomal Aminopeptidase, Microorganism is an enzyme known to target the microsomal aminopeptidase activity. This enzyme plays a crucial role in protein degradation and peptide processing, making it valuable for research in immunology and vaccine development. Its application in the study of parasitic nematodes facilitates advances in molecular vaccines, aiding in the fight against these pathogens. -
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. -
hDHODH Inhibitor
hDHODH-IN-9 is a specific inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 value of 0.34 μM. This compound exhibits significant cytotoxic activity against MCF-7 and A375 cancer cell lines, showcasing its potential for selective targeting in cancer research. hDHODH-IN-9 serves as a valuable tool for studies investigating the role of hDHODH in tumorigenesis and cancer therapy.
