Catalog No.
Product Name
Application
Product Information
Citations
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DPP-4 Inhibitor
DPP-4-IN-15 is a non-competitive inhibitor of dipeptidyl peptidase-4 (DPP-4), exhibiting an IC50 value of 8.24 μM. This compound effectively modulates the activity of DPP-4, an enzyme involved in glucose metabolism and insulin regulation. DPP-4-IN-15 is primarily utilized in diabetes research, providing insights into the potential therapeutic effects of DPP-4 inhibition on glycemic control and related metabolic disorders. -
DPP-III Inhibitor
Fluostatin A is a potent inhibitor of dipeptidyl peptidase III (DPP-III), demonstrating an IC50 value of 0.44 μg/mL with the substrate arginyl-arginine-2-naphthalene formamide. By modulating DPP-III activity, Fluostatin A plays a significant role in studies related to peptide metabolism and signaling pathways. This compound is suitable for research applications in diabetes, cardiovascular disease, and other metabolic disorders targeting DPP-III enzymatic regulation. -
DPP-IV inhibitor
AMG-222 tosylate is a potent DPP-IV inhibitor, primarily employed in the investigation of type II diabetes. By modulating the activity of the DPP-IV enzyme, AMG-222 tosylate facilitates enhanced insulin secretion and improved glycemic control. This compound is valuable for research aimed at understanding the mechanisms of glucose homeostasis and developing therapeutic approaches for managing diabetes. -
DPP-3 Inhibitor
Fluostatin B is a dipeptidyl peptidase 3 (DPP-3) inhibitor with an IC50 value of 24 µg/mL. As a natural product derived from Streptomyces, this compound exhibits potential biological activity in modulating peptide metabolism. Fluostatin B is relevant for research applications focused on understanding DPP-3's role in various physiological processes and exploring its implications in disease states such as diabetes and cancer. -
DPP-4 Inhibitor
H-Gly-Pro-Hyp-OH acetate functions as a dipeptidyl peptidase 4 (DPP-4) inhibitor, exhibiting an IC50 value of 2.51 mM. This compound has shown promise in the investigation of diabetes-related pathways and therapeutic strategies. Its ability to modulate DPP-4 activity makes it a valuable reagent for research in metabolic disorders and glucose homeostasis. -
DPP4 Inhibitor
HTS13517 is a selective inhibitor of Dipeptidyl Peptidase IV (DPP4), exhibiting an IC50 value of 10.73 μM. This compound is relevant for studies investigating the modulation of glucose metabolism and the regulation of incretin hormones. Its applications include diabetes research and the exploration of therapeutic strategies targeting metabolic disorders. -
DPP4 Inhibitor
Garvagliptin is a selective and orally active dipeptidyl peptidase-4 (DPP4) inhibitor, achieving an IC50 of 2.99 nM against human recombinant DPP IV. Its primary mechanism facilitates the enhancement of incretin levels, thereby exhibiting antihyperglycemic effects. Garvagliptin is widely utilized in diabetes research to explore its potential in glycemic control and metabolic regulation. -
Aldose Reductase Inhibitor
Zopolrestat is a potent inhibitor of aldose reductase (AR) with an IC50 of 3.1 nM. This compound is primarily utilized in research focused on diabetic complications, providing insights into the metabolic pathways involved in diabetes-related disorders. Its application extends to studying the therapeutic potential in mitigating diabetic neuropathy and retinopathy, making it a valuable tool in diabetes research. -
Aldose Reductase Inhibitor
Ganoderic acid C2 is a bioactive triterpenoid that functions as an aldose reductase inhibitor, displaying an IC50 of 43.8 µM. This compound exhibits potential anti-tumor activity along with antihistamine and anti-aging properties. Its cytotoxic effects make Ganoderic acid C2 a valuable reagent for research in fields such as cancer biology and metabolic disorders. -
Aldose Reductase Inhibitor
6-Hydroxyluteolin is a flavonoid identified as an aldose reductase inhibitor. It demonstrates potential antidiabetic activity by reducing the conversion of glucose to sorbitol, thereby mitigating osmotic and oxidative stress in diabetic tissues. This compound is useful in research applications focused on diabetes-related complications and metabolic disorders. -
Aldose Reductase Inhibitor
Zenarestat is a potent and orally active inhibitor of aldose reductase, an enzyme involved in the polyol pathway. This compound demonstrates significant biological activity by improving symptoms of diabetic peripheral neuropathy in preclinical models, specifically in Zucker diabetic fatty rats. Zenarestat may serve as a valuable tool for research into diabetic complications and the modulation of glucose-related metabolic disorders. -
Aldose Reductase Inhibitor
Exisulind is an aldose reductase inhibitor with an IC50 of 367 nM in vitro. As an inactive metabolite of sulindac, it may play a role in mitigating complications associated with type 2 diabetes through its pharmacological effects. This compound is valuable for research focused on metabolic disorders and the management of diabetes-related complications. -
Aldose Reductase Inhibitor
Lidorestat is a potent and selective aldose reductase inhibitor, exhibiting an IC50 of 5 nM. This compound is primarily used in research focused on chronic complications associated with diabetes. It has demonstrated efficacy in enhancing nerve conduction and reducing the formation of cataracts, making it valuable for studies relating to diabetic neuropathy and cataractogenesis. -
Aldose reductase Inhibitor
Ganoderic acid C6 functions as an aldose reductase inhibitor, effectively modulating glucose metabolism. This compound is important for research aimed at understanding diabetic complications and oxidative stress management. Its potential to influence pathways associated with diabetic neuropathy and retinopathy makes it a valuable reagent for investigating therapeutic strategies in metabolic disorders. -
ACE/NEP Inhibitor
Fasidotril is a dual inhibitor of neprilysin and angiotensin-converting enzyme (ACE). It demonstrates significant biological activity in the modulation of blood pressure and fluid balance, making it a valuable tool in hypertension and congestive heart failure (CHF) research. The compound's ability to inhibit both pathways provides insight into the therapeutic potential for cardiovascular disease management. -
ACE/NEP Inhibitor
AD015 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin (NEP). It exhibits potent inhibitory activity against NEP, with an IC50 of 0.009 µM, and shows strong inhibition of both nephron ACE (nACE) and cardiac ACE (cACE), with IC50 values of 0.019 µM and 0.0008 µM, respectively. This compound is valuable for research in cardiovascular and renal physiology, particularly in studies related to hypertension and heart failure, where modulation of the renin-angiotensin system is critical. -
NEP Inhibitor
Z-13752A is a mercaptopropanoyl amino acid that functions as an inhibitor of neprilysin (NEP) and angiotensin-converting enzyme (ACE) with Ki values of 1.8 nM and 3.2 nM, respectively. This compound has been shown to effectively reduce arterial blood pressure while enhancing coronary blood flow. Z-13752A is valuable for research focused on coronary artery occlusion and related cardiovascular conditions. -
cACE/NEP Inhibitor
AD011 is a dual inhibitor of carboxypeptidase angiotensin-converting enzyme (cACE) and neprilysin (NEP). This compound is derived from the C-domain selective ACE inhibitor lisinopril-tryptophan and demonstrates significant antihypertensive and cardioprotective effects. AD011 is suitable for research applications focused on cardiovascular health and the modulation of renin-angiotensin system pathways. -
cACE/NEP Inhibitor
AD013 is a dual inhibitor of the enzymes cACE (constitutive Angiotensin-Converting Enzyme) and NEP (Neutral Endopeptidase). This compound is derived from a C-domain selective ACE inhibitor and has demonstrated significant potential in providing antihypertensive and cardioprotective effects. AD013 serves as a valuable reagent for research focused on cardiovascular diseases and hypertension therapies. -
cACE/NEP Inhibitor
AD012 is a dual inhibitor of the enzymes neprilysin (NEP) and angiotensin-converting enzyme (cACE). Designed from the C-domain selective ACE inhibitor, lisinopril-tryptophan, AD012 demonstrates significant antihypertensive and cardioprotective properties. This compound is valuable for research in cardiovascular health and the treatment of hypertension. -
NEP Inhibitor
GW 796406 is a potent neprilysin (NEP) inhibitor with an IC50 value of approximately 1.1-2.5 nM, exhibiting a higher selectivity compared to ACE, which has an IC50 of around 1.6-4.7 nM. This compound is valuable for exploring mechanisms involved in cardiovascular diseases and may aid in the development of therapeutics targeting NEP-related pathways. GW 796406's specificity and efficacy make it a useful tool for researchers studying cardiovascular health and related disorders. -
ACE/NEP Inhibitor
RB-105 is a potent dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), with Ki values of 4.2 nM and 1.7 nM, respectively. By inhibiting ACE, RB-105 decreases angiotensin II production and enhances bradykinin levels, while NEP inhibition further elevates natriuretic peptide levels, resulting in a synergistic increase in bradykinin. This compound exhibits significant antihypertensive and natriuretic effects in both spontaneously hypertensive and normotensive rat models, making RB-105 a valuable reagent for studies on hypertension and related cardiovascular conditions. -
NEP/ACE Inhibitor
Aladotril, a dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE), exhibits potential in ameliorating cardiac hypertrophy without reducing blood pressure. This compound is valuable for research focused on heart failure and the mechanisms of cardiac remodeling following myocardial infarction. Its unique properties make it an important tool for studying cardiovascular health and therapeutic interventions. -
ACE/ECE-1/NEP Inhibitor
CGS 35601 is a potent inhibitor of endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), exhibiting IC50 values of 55 nM, 2 nM, and 22 nM, respectively. This compound effectively suppresses pressor responses induced by big endothelin-1 and angiotensin I, while simultaneously enhancing the circulation of atrial natriuretic peptide (ANP). CGS 35601 serves as a valuable tool in cardiovascular research, particularly in delineating the regulatory mechanisms of cardiovascular function in animal models. -
Angiotensin-Converting Enzyme/Neprilysin Inhibitor
Alatrioprilat is an orally active inhibitor of angiotensin-converting enzyme (ACE) and neprilysin, with an IC50 of 19.6 nM for ACE and 6.1 nM for neprilysin. This compound is significant in the metabolism of hormonal peptides, particularly in the degradation of nitric oxide and atrial natriuretic factor (ANF). Alatrioprilat is applicable in cardiovascular disease research, offering insights into therapeutic strategies for conditions influenced by these pathways. -
Glutamine Synthetase Inhibitor
JFD01307SC is a selective inhibitor of glutamine synthetase, which plays a crucial role in the conversion of L-glutamate to glutamine. By mimicking L-glutamate, JFD01307SC effectively targets and modulates the enzymes involved in glutamine biosynthesis. This compound is primarily utilized in research related to tuberculosis and other metabolic disorders, providing valuable insights into the therapeutic potential of glutamine metabolism modulation. -
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. -
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. -
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. -
Dopamine receptor Agonist, 20S proteasome Activator
Apomorphine hydrochloride is a potent dopamine receptor agonist and a known activator of the 20S proteasome. It enhances proteasomal and insulin-degrading enzyme activities, facilitating the degradation of intracellular amyloid-beta (Aβ), phosphorylated tau (p-tau), and p53, thereby reducing their levels in neuronal cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia. -
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. -
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. -
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.
