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Aldose Reductase Inhibitor
Salfredin B11 is an aldose reductase inhibitor that effectively modulates glucose metabolism by reducing the conversion of glucose to sorbitol. This compound exhibits significant biological activity in the context of diabetic complications, particularly in preventing neuropathy and retinopathy. Salfredin B11 is a valuable tool for research applications focused on the treatment of diabetes-related disorders and the study of oxidative stress responses. -
Aldose Reductase Inhibitor
2-Chloro-1-(4-fluorobenzyl)-1H-benzo[d]imidazole is an aldose reductase (ALR2) inhibitor, demonstrating significant biological activity in modulating glucose metabolism and potentially mitigating diabetic complications. This compound has also shown efficacy in inhibiting larval settlement in marine invertebrates, including barnacles, bryozoans, and polychaetes, while maintaining low toxicity. Its unique properties make it a valuable reagent for research in both diabetes and ecological studies. -
Aldose Reductase Inhibitor
Alrestatin sodium is an aldose reductase inhibitor that plays a significant role in modulating hyperglycemic conditions associated with diabetes mellitus. By inhibiting this enzyme, Alrestatin sodium helps to alleviate oxidative stress and cellular damage, contributing to the prevention of diabetic complications such as neuropathy. This compound is primarily utilized in research focused on diabetes-related pathologies and the development of therapeutic strategies. -
Aldose Reductase Inhibitor
MK181 is an aldose reductase (AR) inhibitor, demonstrating IC50 values of 0.71 μM for aldose reductase and 4.5 μM for AKR1B10. This compound engages the external loop A subpocket of AKR1B10, providing a targeted approach to modulating enzyme activity. MK181 is primarily utilized in research exploring diabetic complications and oxidative stress pathways, making it a valuable tool in pharmacological studies related to metabolic disorders. -
Aldose Reductase Inhibitor
MK 319 is a selective inhibitor of aldose reductase (AR) with an IC50 value of 0.3 μM. This compound is of particular interest in diabetes research, where it may be used to investigate pathways associated with diabetic complications. Additionally, MK 319's role in modulating glucose metabolism can provide insights into therapeutic strategies for managing diabetes and its related disorders. -
Aldose Reductase Inhibitor
Carboxy finasteride is a significant metabolite of the 5α-reductase inhibitor finasteride, targeting aldose reductase. As a biotransformation product of finasteride, it is primarily formed through oxidation by cytochrome P450 (CYP3A4) and represents the predominant metabolite found in urine, while hydroxy finasteride is more prevalent in plasma. This compound plays a crucial role in research related to metabolic pathways and the pharmacokinetics of finasteride, contributing to studies on diabetic complications and related enzymatic activities. -
Aldose Reductase Inhibitor
M79175 is an aldose reductase inhibitor that plays a crucial role in the management of diabetic complications. By inhibiting the enzyme, M79175 assists in the reduction of sorbitol accumulation, which is implicated in the pathogenesis of diabetic retinopathy. This reagent is relevant for researchers investigating early stages of diabetic retinopathy and potential therapeutic strategies for diabetes-related ocular disorders. -
Aldose Reductase Inhibitor
AL-4114 is a potent aldose reductase inhibitor that plays a critical role in the management of diabetic complications. This compound has demonstrated significant biological activity in the prevention of diabetic cataractogenesis, making it valuable for research focused on diabetes-related ocular disorders. Its application extends to the investigation of metabolic pathways and the development of therapeutic strategies for diabetes management. -
Aldose Reductase Inhibitor
ALO1567 is an orally available aldose reductase inhibitor that demonstrates an IC50 of 27 nM against rat lens aldose reductase. This compound is utilized in research focused on diabetes, particularly in studying the pathways related to hyperglycemia and osmotic stress in diabetic complications. Its specific targeting of aldose reductase makes it a valuable tool for investigating therapeutic strategies in metabolic disorders. -
Aldose Reductase Inhibitor
Salfredin A7 is an aldose reductase inhibitor that targets the enzyme responsible for converting glucose into sorbitol. This activity is significant in the context of diabetic complications, where the accumulation of sorbitol leads to cellular damage. Salfredin A7 exhibits anti-inflammatory properties and has potential applications in research focusing on diabetes-related pathologies and oxidative stress. Its inhibitory action on aldose reductase makes it a valuable reagent for studies investigating metabolic diseases and their associated complications. -
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. -
DHODH Inhibitor
DSM502 is a pyrrole-based inhibitor targeting Dihydroorotate Dehydrogenase (DHODH). It demonstrates nanomolar potency against Plasmodium DHODH and effectively inhibits Plasmodium parasites while showing no activity against mammalian DHODHs. This selectivity makes DSM502 a valuable tool for research into malaria and other Plasmodium-related diseases. -
Proteasome Inhibitor
LXE408 is an orally active, non-competitive inhibitor of the proteasome, exhibiting selective action against kinetoplastids. With an IC50 of 0.04 μM for the L. donovani proteasome, LXE408 effectively inhibits parasite proliferation, demonstrated by an EC50 of 0.04 μM against L. donovani. Due to its limited ability to cross the blood-brain barrier, LXE408 is particularly suitable for research focused on visceral leishmaniasis (VL). -
Kinetoplastid Proteasome Inhibitor
GNF6702 is a selective inhibitor of the kinetoplastid proteasome, targeting the degradation pathway critical for parasite survival. This compound demonstrates potent activity against various kinetoplastid parasites and has shown efficacy in clearing infections in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis. GNF6702 is valuable for research focused on developing therapies for these neglected tropical diseases. -
DHODH Inhibitor
DSM705 hydrochloride is a potent inhibitor of Dihydroorotate Dehydrogenase (DHODH), targeting the enzymatic activity essential for the de novo pyrimidine synthesis in Plasmodium species. It demonstrates high nanomolar potency against P. falciparum and P. vivax DHODH with IC50 values of 95 nM and 52 nM, respectively, while sparing mammalian DHODH enzymes. This compound is valuable for research into antimalarial therapeutics and understanding the biochemical mechanisms of Plasmodium infections. -
L. donovani Proteasome Inhibitor
GSK3494245 is a selective inhibitor of the chymotrypsin-like activity of the Leishmania donovani proteasome, targeting a site between the β4 and β5 subunits with an IC50 of 0.16 μM. This compound demonstrates moderate inhibitory effects on the chymotrypsin-like activity of human proteasomes, exhibiting IC50 values of 13 µM in purified 26S and 40 µM in enriched THP-1 extracts. GSK3494245's potent activity and favorable biosafety profile make it a valuable tool for research in parasitology and potential therapeutic applications against leishmaniasis. -
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. -
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. -
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. -
Tyrosinase inhibitor
Aloin (Barbaloin) is a yellow crystalline substance obtained from aloe and is reported to be a potent inhibitors of tyrosinase.

