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Tyrosinase Inhibitor
Polyphyllin C is a spirostanol saponin that acts as a tyrosinase inhibitor. It demonstrates mild inhibitory activity against tyrosinase with an IC50 of 36.87 µM. Additionally, Polyphyllin C exhibits moderate antileishmanial effects, with an IC50 of 1.59 µg/mL, making it a candidate for research in skin pigmentation disorders and leishmaniasis treatment. -
PfDHODH Inhibitor
PfDHODH-IN-2 is a specific inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH), exhibiting potent activity with an IC50 of 1.11 µM. This compound serves as an effective antimalarial agent, making it valuable for research focused on malaria and the development of therapeutic strategies against this disease. Its mechanism of action targets the pyrimidine biosynthesis pathway, providing a crucial approach for disrupting parasite proliferation. -
DHODH Inhibitor
DSM705 is a pyrrole-based inhibitor of Dihydroorotate Dehydrogenase (DHODH). It demonstrates nanomolar potency against Plasmodium DHODH and exhibits significant activity against Plasmodium parasites while sparing mammalian DHODHs. This compound is a potent antimalarial agent, making it a valuable tool for research in malaria treatment and related studies. -
HCV Protease Inhibitor
MK-2748 is a potent inhibitor of the hepatitis C virus (HCV) NS3/4A protease. It demonstrates broad-spectrum antiviral activity across all genotypes (gt1a-gt6) with nanomolar potency (IC₅₀ < 0.115 nM), including strong efficacy against drug-resistant mutant strains such as gt1b R155K (IC₅₀ = 0.032 nM) and D168Y (IC₅₀ = 0.057 nM). MK-2748 is valuable for research on HCV infection and contributes to the understanding of antiviral mechanisms and treatment strategies. -
HCV Protease Inhibitor
AL-611 is an inhibitor of the Hepatitis C virus (HCV) NS5B polymerase, demonstrating potent activity with an EC50 value of 5 nM. This compound plays a critical role in antiviral research, particularly in the development of therapeutic strategies against HCV infections. Its effectiveness in inhibiting HCV replication makes it a valuable tool for studies focused on viral RNA synthesis and enzyme interactions. -
HCV Protease Inhibitor
GSK2818713 is a selective Hepatitis C virus (HCV) protease inhibitor that disrupts the replication complex associated with the NS5A protein. This compound exhibits potent anti-HCV activity, making it a valuable tool for studying the replication and life cycle of the virus. GSK2818713 is applicable in research focused on developing therapeutic strategies against Hepatitis C. -
HCV Protease Inhibitor
BI-1230 is a potent inhibitor of the HCV NS3 protease, exhibiting nanomolar activity in blocking viral replication. It demonstrates high selectivity against other serine and cysteine proteases, making it a valuable tool for studying hepatitis C virus infection mechanisms. Additionally, BI-1230 shows favorable pharmacokinetic properties, supporting its potential use in drug development and research applications related to antiviral therapy. -
HCV Protease Inhibitor
MK-6169 is a potent hepatitis C virus (HCV) protease inhibitor that targets the viral NS5A protein. It exhibits broad-spectrum activity against various HCV genotypes, making it a valuable tool for research on antiviral therapies in hepatitis C. This compound is useful for exploring the mechanisms of HCV replication and potential treatment strategies in pharmaceutical development. -
HCV Protease Inhibitor
Isoeuphorbetin is a dimeric coumarin that acts as a potent inhibitor of HCV protease, demonstrated by an IC50 value of 3.63 µg/mL. This compound has significant potential in antiviral research, particularly in the development of therapeutics targeting hepatitis C virus infection. Its ability to effectively block viral protease activity makes it a valuable tool for studying HCV biology and drug discovery. -
HCV Protease Inhibitor
Ac-D-DGla-LI-Cha-C is a potent inhibitor of the hepatitis C virus (HCV) protease, effectively disrupting viral replication. This peptide is instrumental in studying various biological processes and diseases, including cancer, autoimmune disorders, fibrotic conditions, inflammatory responses, neurodegenerative diseases, infectious diseases, lung and cardiovascular disorders, as well as metabolic diseases. Its targeted action on HCV protease makes it a valuable tool for research in virology and therapeutic development. -
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. -
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. -
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. -
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. -
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 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. -
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. -
L-glutamine Analog
Azotomycin is an L-glutamine analog that exhibits antitumor activity through the modulation of cellular metabolism and signaling pathways. This compound serves as a valuable tool in cancer research, particularly in studies focusing on glutamine metabolism and its implications in tumor growth and proliferation. Researchers may utilize Azotomycin to investigate therapeutic strategies targeting glutamine-dependent cancer cells. -
L-glutamine antagonist
NSC 303861 is an L-glutamine receptor antagonist that selectively inhibits glutamine-dependent enzymes involved in purine nucleotide synthesis while sparing pyrimidine synthase. This compound exhibits significant cytotoxic effects against liver cancer 3924A cells, with an LC50 of 6 µM. NSC 303861 is valuable for cancer research, particularly in studies focused on targeting metabolic pathways in malignancies. -
Tyrosinase Inhibitor
p-Coumaric Acid Ethyl Ester serves as a non-competitive, reversible inhibitor of tyrosinase, with an IC50 value of 4.89 μg/mL and a Ki of 1.83 μg/mL. This compound quells the intrinsic fluorescence of the enzyme and alters the binding affinity of L-tyrosine by inducing conformational changes within the catalytic domain without interfering with the copper ion binding. p-Coumaric Acid Ethyl Ester has applications in the development of pharmaceuticals, cosmetics, and fruit preservation products. -
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.

