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Catalog No.
Product Name
Application
Product Information
Citations
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Tyrosinase Inhibitor
Methyl cinnamate (Methyl 3-phenylpropenoate) is an effective tyrosinase inhibitor, primarily utilized to prevent enzymatic browning in food products. In addition to its role in food applications, it demonstrates antimicrobial properties and exhibits antiadipogenic effects, partly mediated by the CaMKK2-AMPK signaling pathway. This compound is valuable for researchers exploring therapeutic strategies in skin pigmentation disorders and metabolic regulation. -
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. -
Aminopeptidase P2 Inhibitor
ST-115 is a potent inhibitor of aminopeptidase P2, a target involved in the regulation of various physiological processes. Its high specificity makes it an invaluable tool for studying the role of aminopeptidase P2 in ischemic stroke and related conditions. Researchers may utilize ST-115 to explore its potential therapeutic implications in neuroprotection and recovery following cerebral ischemia. -
Aminopeptidase A Inhibitor
Firibastat is a potent inhibitor of aminopeptidase A (APA), exhibiting a Ki value of 200 nM. This first-in-class compound effectively inhibits the conversion of brain angiotensin-II to angiotensin-III, resulting in reduced blood pressure in hypertensive models. Firibastat is particularly valuable in exploring the role of APA in neurophysiological processes and hypertension research. -
Aminopeptidase Inhibitor
L-Leucinol is a competitive inhibitor of aminopeptidase, exhibiting a Ki value of 17 μM. This reagent is primarily utilized in in vitro enzymatic assays to study enzymatic activity and inhibition. Additionally, L-Leucinol serves as a valuable tool in peptide synthesis applications, facilitating the exploration of peptide structure and function in biochemical research. -
Aminopeptidase/Epoxide Hydrolase Inhibitor
ARM1 (4BSA) is a potent inhibitor of aminopeptidase and epoxide hydrolase. It exhibits aminopeptidase inhibitory activity with an IC50 of 7.61 µM and demonstrates epoxide hydrolase inhibitory activity with an IC50 of 12.4 µM. This compound is valuable for research applications targeting metabolic pathways involving peptide and epoxide metabolism. -
Anti-inflammatory Agent, Aminopeptidase Inhibitor
2-(2'-Pyridyl)benzimidazole is an effective anti-inflammatory agent and a potent inhibitor of methionine aminopeptidase in Escherichia coli. This compound exhibits tridentate ligand properties, capable of forming stable complexes with various transition metal ions. Its applications extend to biochemical research focused on inflammatory processes and amino acid metabolism, making it a valuable reagent for studies in these areas. -
Leucine Aminopeptidase Inhibitor
Adamantanine is a potent inhibitor of leucine aminopeptidase, demonstrating an I/S0.5 value of 10.5. It effectively impairs the transport of methionine and leucine in Ehrlich ascites carcinoma cells, with a Ki value of 0.76 mM. Additionally, Adamantanine displays inhibitory effects on the proliferation of P388 lymphocytic leukemia cells, exhibiting an IC50 of greater than 1 mM. This compound serves as a valuable tool for researchers investigating amino acid transport and cancer cell proliferation. -
Neutral Endopeptidase Inhibitor, Aminopeptidase N Inhibitor
RB 101 is a mixed inhibitor of neutral endopeptidase and aminopeptidase N, enzymes that metabolize enkephalins. This compound exhibits long-lasting antinociceptive effects and inhibits in vivo [3H]DPN binding in mice under both basal conditions and after swim stress. RB 101 is particularly useful for studying the in vivo localization of enkephalinergic pathways activated by various stimuli, making it a valuable tool for pain research and neuropharmacology. -
Aminopeptidase B Inhibitor
Arphamenine A is a potent inhibitor of aminopeptidase B, derived from Chromobacterium violaceum HMG361-CF4. This compound has demonstrated the ability to inhibit aminopeptidase B activity, contributing to its potential anticancer effects. Research indicates that Arphamenine A may suppress the growth of sarcoma 180 and invasive micropapillary carcinoma (IMC), making it a valuable tool for studying cancer biology and therapeutic strategies targeting aminopeptidase B. -
Aminopeptidase N Inhibitor
Aminopeptidase N Inhibitor 1 is a potent inhibitor targeting aminopeptidase N, demonstrating an IC50 of 25 μM. It plays a significant role in research related to tumor angiogenesis, providing valuable insights into the mechanisms of cancer progression and the development of therapeutic strategies. Its application in studies of angiogenesis makes it a crucial tool for researchers investigating tumor microenvironment interactions. -
Leukotriene A4 Hydrolase Inhibitor
JNJ-26993135 is a selective inhibitor of leukotriene A4 hydrolase (LTA4H), demonstrating an IC50 value of 11 nM. This compound is valuable for research applications focusing on inflammatory processes and leukotriene metabolism. Its ability to modulate leukotriene synthesis suggests potential use in studying various inflammatory diseases and related therapeutic interventions. -
Aminopeptidase N Inhibitor
Probestin is a potent inhibitor of aminopeptidase N (APN), derived from the bacterium Streptomyces cyanogens MH663-2F6. This compound exhibits significant biological activity by selectively blocking APN activity, leading to the modulation of various physiological processes. Probestin is valuable for research applications focused on studying the role of APN in cancer, inflammation, and immune response pathways. -
Aminopeptidase-M Inhibitor
Leuhistin is an aminopeptidase-M (AP-M) inhibitor, targeting the enzymatic degradation of bioactive peptides within cerebral membranes. By inhibiting AP-M, Leuhistin enhances the availability and activity of these peptides, making it a valuable reagent for studies focused on neurobiology and peptide research. It is derived from Bacillus laterosporus BMI156-14F1, highlighting its natural origins in biochemical applications. -
Leukotriene A4 Hydrolase Inhibitor
LTA4H-IN-2 is a potent inhibitor of Leukotriene A4 Hydrolase, demonstrating an IC50 of less than 3 nM. This compound plays a crucial role in modulating inflammatory responses by inhibiting the biosynthesis of leukotrienes, which are key mediators in various inflammatory diseases. LTA4H-IN-2 is valuable for research applications focused on understanding leukotriene signaling pathways and developing therapeutics for conditions such as asthma and other inflammatory disorders. -
Aminopeptidase Inhibitor
Matlystatin A is a potent inhibitor of aminopeptidases, exhibiting IC50 values of 0.3 μM and 0.56 μM against 92 kDa and 72 kDa type IV collagenases, respectively. This compound is valuable for investigating proteolytic processes in cancer research. Its ability to modulate enzymatic activity provides insights into tumor progression and metastasis mechanisms. -
Aminopeptidase Inhibitor
Ketomethylenebestatin is a selective inhibitor of aminopeptidases, showcasing notable activity against AP-B, AP-M, and Leu-AP with IC50 values of 56 μM, 752 μM, and 0.39 μM, respectively. This compound serves as an analog of the natural aminopeptidase inhibitor Bestatin, and is valuable in research applications focused on the regulation of peptide metabolism and potential therapeutic targets in various diseases. Its specificity towards aminopeptidases makes it a useful tool for investigating enzymatic pathways and the role of these enzymes in physiological processes. -
Aminopeptidase Inhibitor
Lys-psi(CH2NH)-Trp(Nps)-OMe is a pseudodipeptide analog of lysine and tryptophan designed to inhibit aminopeptidase activity. This compound exhibits significant analgesic properties, demonstrated through dose-dependent and naloxone-reversible responses following intracerebroventricular administration in murine models. It not only prolongs analgesic effects compared to its parent compound but also offers protection against the degradation of methionine enkephalin in rat striatal slices. Lys-psi(CH2NH)-Trp(Nps)-OMe's enhanced resistance to proteolysis contributes to its sustained analgesic activity, making it a valuable tool for studying pain mechanisms and the role of aminopeptidases in neuromodulation. -
μ-Calpain Inhibitor
Calpain Inhibitor-2 is a peptide inhibitor targeting μ-calpain, with a Ki value of 9 nM. This compound demonstrates significant antiproliferative activity against melanoma cell lines, specifically A-375 and B-16F1, as well as PC-3 prostate cancer cells in vitro. It is a valuable tool for research applications focused on exploring calpain-mediated pathways in cancer biology. -
PREP Inhibitor
Y-29794 is a selective, orally active inhibitor of non-peptide prolyl endopeptidase (PREP), demonstrating an IC50 of 3 nM and a Ki of 0.95 nM. It enhances the efficacy of thyrotropin-releasing hormone (TRH) on acetylcholine release in the rat hippocampus, indicating potential neuroprotective effects. Additionally, Y-29794 exhibits anticancer activity by inhibiting the IRS1-AKT-mTORC1 signaling pathway and shows the capability to penetrate the blood-brain barrier (BBB), making it valuable for various neurological and oncology research applications. -
Prolyl Endopeptidase Inhibitor
Z-Thioprolyl-Thiazolidine is a potent and selective inhibitor of prolyl endopeptidase, exhibiting a Ki value of 0.36 nM for bovine brain prolyl endopeptidase. This compound is valuable for research applications focused on peptide metabolism and neuropeptide regulation. Its specificity makes it an essential tool for studying the physiological and pathological roles of prolyl endopeptidase in various biological systems. -
POP Inhibitor
POP-IN-1 is a potent inhibitor of prolyl oligopeptidase (POP), exhibiting a Ki value of 0.009 μM. This compound demonstrates significant inhibitory activity, making it valuable for research related to neurodegenerative diseases and cancer progression. Its ability to modulate POP activity provides a valuable tool for investigating therapeutic strategies in these critical areas of study. -
Prolyl Endopeptidase (PREP) Inhibitor
Z-Pro-Pro-aldehyde-dimethyl acetal is a highly selective inhibitor of prolyl endopeptidase (PREP), a serine endoprotease located in the cytoplasm, with an IC50 value of 12 nM. This compound is vital for investigating cognitive dysfunction associated with aging and neurodegenerative diseases such as Alzheimer's disease. Its ability to modulate PREP activity makes it a valuable tool for research in neurobiology and related therapeutic areas. -
NEP Inhibitor
CGS 24592 is a selective and potent inhibitor of neutral endopeptidase 24.11 (NEP), exhibiting an IC50 value of 1.6 nmol/L. This compound effectively decreases the degradation of atrial natriuretic peptide (ANP), leading to increased plasma levels of ANP and subsequent reduction in blood pressure. CGS 24592 is valuable for research in cardiovascular diseases, particularly in the contexts of hypertension and congestive heart failure. -
PREP Inhibitor
Linderene acetate is a prolyl endopeptidase (PREP) inhibitor derived from the root of Lindera strychnifolia. This compound exhibits significant biological activity in modulating peptide metabolism and has potential applications in neurodegenerative research, where PREP plays a role in the regulation of neuropeptides. Its inhibition may offer insights into therapeutic strategies for disorders related to dysregulated peptide processing. -
PREP Inhibitor
ARI-3531 is a selective inhibitor of prolyl oligopeptidase (PREP), exhibiting a Ki of 0.73 nM. This compound is valuable for investigating the mechanisms underlying tumor invasion and metastasis, enabling enhanced understanding of cancer progression and potential therapeutic interventions. -
Prolyl Endopeptidase Inhibitor
Z-Thioprolyl-Thioproline is a selective inhibitor of prolyl endopeptidase (PEP), exhibiting an IC50 of 16 µM and a Ki of 37 µM. This compound is utilized in research focused on neurological disorders, particularly pertaining to memory and cognitive impairments. Its ability to modulate PEP activity makes it a valuable tool for investigating potential therapeutic strategies for these conditions. -
POP Inhibitor
POP-IN-3 is a potent, covalent inhibitor of prolyl oligopeptidase (POP), exhibiting a Ki of 0.95 nM. This compound is valuable for research into neurodegenerative diseases and cancer, as it modulates the activity of POP, an enzyme implicated in cellular signaling and disease progression. It is suitable for in vitro and in vivo studies to explore the therapeutic potential of targeting POP in various pathological conditions. -
PREP Inhibitor
JTP-4819 is a highly selective inhibitor of prolyl endopeptidase (PREP), exhibiting potent inhibition with IC50 values of 0.83 nM in rat brain supernatant and 5.43 nM in Flavobacterium meningosepticum. This compound demonstrates significant blood-brain barrier penetration, making it relevant for neuropharmacological studies. JTP-4819 has shown promise in enhancing memory retention in amnesia models induced by scopolamine, supporting its applications in cognitive research and potential therapeutic development for memory disorders. -
PREP Inhibitor
Z-Pro-prolinal is a potent inhibitor of prolyl endopeptidase (PREP), exhibiting an IC50 value of 0.4 nM for porcine PREP. This compound is characterized by its oral bioavailability and specificity, making it a valuable tool for investigating PREP's role in physiological processes. Research applications include studying neuropeptide metabolism and potential therapeutic interventions in neurodegenerative diseases. -
Prolyl Endopeptidase Inhibitor
Poststatin is a selective inhibitor of prolyl endopeptidase (PEP), a key enzyme involved in the degradation of bioactive peptides such as bradykinin. By inhibiting PEP, Poststatin enhances the levels of bradykinin, which may play a crucial role in modulating pain and inflammation. This reagent is valuable for research applications focused on pain pathways, inflammatory responses, and cardiovascular regulation. -
Prolyl Endopeptidase Inhibitor
Kynapcin-13 is a non-competitive inhibitor of prolyl endopeptidase (PEP), exhibiting an IC50 of 76.80 μM. It selectively targets PEP with minimal inhibition of other serine proteases. This compound is valuable for research applications investigating the role of PEP in various physiological processes and its implications in neurodegenerative diseases. -
Prolyl Endopeptidase Inhibitor
Polyozellin is a potent prolyl endopeptidase inhibitor known for its capacity to modulate proteolytic activity. This compound demonstrates significant anti-inflammatory, anticancer, and antioxidant properties, making it a valuable tool in the study of various disease mechanisms. Its application extends to research on inflammation, cancer therapy, and the management of oxidative stress-related disorders. -
Prolyl Endopeptidase Inhibitor
Kynapcin-28 is a non-competitive inhibitor of prolyl endopeptidase (PEP), demonstrating an IC50 value of 76.80 μM. This compound selectively inhibits PEP while exhibiting minimal effects on other serine proteases. Kynapcin-28 is valuable for studying protein metabolism and has potential applications in neurodegenerative disease research, where PEP modulation may play a critical role. -
Prolyl Endopeptidase Inhibitor
Eurystatin A is a selective inhibitor of prolyl endopeptidase, an enzyme involved in the cleavage of proline-containing peptides. This compound exhibits significant biological activity by modulating peptide metabolism, which has implications in various physiological processes. Research applications include studying the role of prolyl endopeptidase in neurodegenerative diseases and exploring its potential therapeutic effects in related disorders. -
PED Inhibitor
Eurystatin B is an inhibitor of prolyl endopeptidase (PED), a crucial enzyme involved in peptide metabolism. It demonstrates protective effects against memory impairment induced by scopolamine in rodent models, indicating potential applications in cognitive research and neuroprotection studies. This compound may be valuable for investigating mechanisms underlying memory disorders and developing therapeutic strategies. -
Chymase Inhibitor
6-Chlorooxindole is a selective chymase inhibitor, exhibiting an IC50 of 470 μM. This compound demonstrates over 100-fold selectivity for chymase compared to cathepsin G. 6-Chlorooxindole is valuable for research applications focused on cardiovascular disease mechanisms and therapeutic interventions. -
Vimentin Inhibitor
Vimentin-IN-1 is a selective vimentin inhibitor that acts by binding to the type III intermediate filament protein, vimentin (VIM). This binding induces hyperphosphorylation at Ser56, leading to the selective disruption of mitosis and consequent multinucleation in vimentin-expressing mesenchymal cancer cells. Vimentin-IN-1 demonstrates improved oral bioavailability and favorable pharmacokinetic properties compared to its precursor, FiVe1, making it a valuable tool for cancer research applications focused on targeting vimentin-related pathways. -
Vimentin Inhibitor
FiVe1 is a potent inhibitor of vimentin (VIM), targeting its rod domain to induce disassembly and hyperphosphorylation at Ser56. This mechanism results in mitotic catastrophe, multinucleation, and a loss of stemness in cancer cells. FiVe1 demonstrates anticancer effects, particularly against soft tissue sarcomas, and enhances the sensitivity of ovarian cancer cells to Cisplatin. This compound is valuable for research involving mesenchymal cancers, such as breast cancer and soft tissue sarcoma, as well as ovarian cancers. -
Calpain Inhibitor
PD 151746 is a potent calpain inhibitor that demonstrates 20-fold selectivity for u-calpain, with a reported inhibition constant (Ki). This compound is primarily utilized in research to study the role of calpain in various biological processes, including calcium-regulated proteolysis and cellular signaling pathways. Its effectiveness makes it a valuable tool for investigating calpain's contribution to diseases such as neurodegeneration and cardiac dysfunction. -
Immunoproteasome Inhibitor
Zetomipzomib maleate is a first-in-class immunoproteasome inhibitor that selectively targets the LMP7 and LMP2 subunits, demonstrating IC50 values of 39 nM and 131 nM, respectively. This compound is primarily utilized in the study of autoimmune diseases, where it may modulate immune responses by inhibiting immunoproteasome activity. Its distinct mechanism offers a valuable tool for researchers investigating the pathological roles of the immunoproteasome in various disorders. -
Diabetogenic Agent/Proteasome Inhibitor
Alloxan hydrate is a diabetogenic agent that induces diabetes by selectively destroying insulin-secreting beta cells in the pancreas. Additionally, it acts as a proteasome inhibitor, disrupting protein degradation pathways. This compound is widely utilized in research to study diabetes mechanisms and the role of proteasome activity in cellular processes. -
Calpain-2 Inhibitor
NA-184 is a selective calpain-2 inhibitor, demonstrating an IC50 of 134 nM against mouse calpain-2, with minimal activity towards calpain-1 (IC50 of 2826 nM). This compound exhibits significant neuroprotective properties, making it a valuable tool for research on traumatic brain injury (TBI). Additionally, NA-184 shows limited inhibition of other protease classes, underscoring its specificity in experimental settings. -
MuRF1 Inhibitor
MyoMed 205 is a potent MuRF1 inhibitor that functions by preventing the ubiquitination and proteasomal degradation of skeletal muscle proteins. This compound enhances muscle performance and mitigates muscle wasting and weight loss associated with various conditions. MyoMed 205 is suitable for research applications related to cancer cachexia, type 2 diabetes mellitus, and heart failure with preserved ejection fraction, making it a valuable tool in understanding muscle atrophy and metabolic disorders. -
Calpain-2 Inhibitor
Calpain-2-IN-1 is an isoform-specific inhibitor targeting calpain-2, exhibiting a Ki of 7.8 nM for calpain-2 and 181 nM for calpain-1. This selective inhibition allows for precise modulation of calpain-2 activity, making it a valuable tool in the study of neurodegenerative diseases and disorders affecting synaptic function. Its application in research provides insights into the role of calpain-2 in various cellular processes and disease mechanisms. -
Immunoproteasomes Inhibitor
LU-005i is a potent inhibitor of the β5i subunit of immunoproteasomes, demonstrating an IC50 of 6.6 nM and selectivity over the β5c subunit with an IC50 of 287 nM. This compound is valuable for research into modulation of immune responses and antigen processing, offering insights into autoimmune diseases and cancer immunotherapy. Its specificity for immunoproteasomes makes it a useful tool for studying the role of proteasomal pathways in various biological processes. -
20S Proteasome Inhibitor
5-Amino-8-hydroxyquinoline is a non-competitive inhibitor of the 20S proteasome, demonstrating potent inhibitory effects on NF-κB activity. This compound induces apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. It is valuable for research applications in cancer biology, particularly in the study of leukemia and related malignancies. -
Calpain Inhibitor
Dazcapistat is an orally active small-molecule inhibitor targeting calpain 1, 2, and 9. This compound significantly reduces the expression and production levels of IL-6 in injured lung tissue, contributing to decreased fibrosis. Dazcapistat exhibits anti-fibrotic properties in various animal models, including those for skin, liver, and lung fibrosis. Its applications extend to research on coronavirus disease 2019 (COVID-19) and idiopathic pulmonary fibrosis. -
Immunoproteasome Inhibitor
Zetomipzomib is a selective inhibitor of the immunoproteasome, specifically targeting the LMP7 and LMP2 subunits with reported IC50 values of 39 nM and 131 nM, respectively. This first-in-class compound demonstrates significant potential in the investigation of autoimmune diseases, providing a valuable tool for research into the modulation of immune responses and proteasomal degradation pathways. Researchers can utilize Zetomipzomib to explore therapeutic avenues for conditions where the immunoproteasome plays a critical role. -
Proteasome Inhibitor
LU-002i is a selective inhibitor of the β2c and β2i subunits of the human proteasome, exhibiting an IC50 of 220 nM for the β2i subunit. This compound is valuable for research applications involving protein degradation and cellular stress responses. Its specific targeting can aid in the elucidation of proteasome-related pathways and the development of therapeutic strategies for conditions influenced by proteasome activity.
