Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Prolyl Endopeptidase (PREP)
Ala-Ala-βNA is a dipeptidyl-fluoronaphthylamide (βNA) that primarily targets prolyl endopeptidase (PREP). This compound undergoes efficient hydrolysis, demonstrating optimal activity at a pH range of 8.5 to 9.0. Ala-Ala-βNA is valuable for studying the enzymatic mechanisms of PREP and assessing its role in various biological processes, making it an essential reagent for biochemical research applications. -
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. -
Proteasome Assembly Modulator
TCH-165 is a small molecule proteasome assembly modulator that enhances the levels of the 20S proteasome. This compound facilitates 20S-mediated protein degradation, making it a valuable tool for studying protein turnover and homeostasis. TCH-165 is applicable in research involving cancer biology, neurodegenerative diseases, and cellular stress responses. -
20S Proteasome Activator
20S Proteasome Activator 1 is a potent activator of the 20S proteasome, demonstrating effective EC200 values of 0.3 μM, 0.7 μM, and 1.8 μM for trypsin-like, chymotrypsin-like, and caspase-like activities, respectively. This compound functions effectively within cellular environments, mitigating the accumulation of the pathogenic A53T mutant of α-synuclein. It is particularly useful for research in the context of neurodegenerative diseases, facilitating studies on proteostasis and related therapeutic approaches. -
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. -
Proteasome Substrate
Z-Ala-Arg-Arg-AMC is a fluorogenic proteasome substrate designed to specifically assay the trypsin-like activity of the proteasome. Its unique structure allows for sensitive detection of proteolytic activity, making it a valuable tool for studying protein degradation and turnover in cellular processes. This substrate is widely utilized in research applications focused on proteasome function and its implications in various diseases. -
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. -
LMP2 Fluorogenic Substrate
Ac-PAL-AMC is a fluorogenic substrate specifically designed for the 20S proteasome LMP2/β1i activity. It is utilized in biochemical assays to monitor proteasomal degradation processes, facilitating research into protein turnover and associated cellular functions. This substrate can enable real-time measurement of protease activity, making it an essential tool for studies in cancer, neurodegeneration, and other diseases linked to proteostasis. -
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. -
26S Proteasome Substrate
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate designed for the 26S proteasome, targeting its catalytic activities. This compound is utilized primarily for assessing the caspase-like activity of the 26S proteasome in various biological studies. Its application is crucial for understanding proteasomal regulation and function in cellular processes. -
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. -
Arg Tag
Boc3Arg is a tert-butyl carbamate-protected form of arginine, designed to facilitate protein degradation by targeting the 20S proteasome. Its unique properties enable efficient localization of tagged proteins for proteasomal degradation, making it a valuable tool in studies of protein turnover and regulation. Boc3Arg is particularly useful in research applications that investigate ubiquitin-proteasome pathways and protein quality control mechanisms in cells. -
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. -
26S Proteasome Substrate
Ac-RLR-AMC is a fluorogenic substrate specifically designed for the 26S proteasome pathway. Upon proteolytic cleavage, the release of 7-amino-4-methylcoumarin (AMC) generates fluorescence, facilitating the quantification of trypsin-like activity within the proteasome. This reagent is valuable for research applications focused on proteasome function, cellular regulation, and related biochemical assays. -
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. -
Immunoproteasome β5i Subunit Inhibitor
DPLG3 is a selective inhibitor of the immunoproteasome β5i subunit, demonstrating an IC50 of 4.5 nM. It effectively inhibits the mouse i-20S proteasome with an IC50 value of 9.4 nM. DPLG3 is capable of downregulating the protein levels of NF-κB p50 and p65, highlighting its potential in the study of immune-related diseases and therapeutic applications. -
Proteasome Inhibitor
BC-23 (NSC 45382) is a potent proteasome inhibitor that selectively inhibits the chymotrypsin-like (CT-L) activity of the proteasome complex. This compound demonstrates significant cytotoxicity against malignant cells while sparing normal cells, making it a valuable tool for cancer research. BC-23 is utilized in studies aimed at elucidating the role of proteasomal degradation in cell cycle regulation and tumor progression. -
Immunoproteasome Activator
Immunoproteasome Activator 1 is a selective activator of the immunoproteasome that enhances the presentation of MHC-I-bound peptides by over 100-fold. This compound functions by binding to the proteasome structural subunit PSMA1, facilitating the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes. Its significant biological activity makes it valuable for research focused on immune response modulation and antigen processing. -
Proteasome Subunit Binder
Biotin-epoxomicin is a proteasome subunit binder that serves as an affinity reagent for the identification and purification of proteasomal catalytic subunits. This compound enables the affinity purification of active subunits, facilitating their subsequent analysis via liquid chromatography-mass spectrometry (LC-MS). Biotin-epoxomicin is particularly useful in research applications focused on solid tumors, such as those derived from B16 melanoma, providing insights into proteasome function in cancer biology. -
Thrombin Inhibitor
Thrombin Inhibitor 5 is a potent thrombin inhibitor, exhibiting IC50 values between 0.1 μM and 1 μM. This compound demonstrates significant biological activity in the modulation of thrombin activity, making it a valuable tool in researching venous thromboembolism and related coagulation disorders. Its efficacy allows for potential applications in understanding thrombotic mechanisms and developing therapeutic interventions. -
calpain I Inhibitor
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I, exhibiting a binding affinity of Ki=19 nM. This compound displays reduced binding to calpain II (Ki=120 nM) and cathepsin B (Ki=750 nM), making it a valuable tool for dissecting calpain-related biochemical pathways. Its applications span various fields, including studies on neutrophil chemotaxis, neuronal signaling, and cardiac responses to injury, facilitating insights into calpain's role in cellular processes and pathologies. -
20S Proteasome Substrate
Z-Leu-Leu-Leu-AMC is a fluorogenic substrate designed for the assessment of chymotrypsin-like protease activity in the 20S proteasome. It provides a sensitive and specific means to monitor proteasomal function and proteolytic activity. This reagent is valuable for research applications involving protein degradation, cellular homeostasis, and the study of proteasome-related diseases. -
Proteasome Inhibitor
Biotin-(Oaa)3-epoxomicin is a biotinylated proteasome inhibitor derived from Epoxomicin, connected through three hydrophilic oxaacetyl amino acid linkers. This compound is utilized primarily in proteomic research for the capture and identification of proteasome complexes, facilitating target validation and elucidation of intracellular targets. Epoxomicin effectively inhibits proteasome activity through covalent binding to catalytic subunits such as LMP7, X, MECL1, and Z, with a pronounced effect on chymotrypsin-like activity, while sparing non-proteasomal proteases like trypsin and papain. Additionally, it serves as an NF-κB inhibitor, demonstrating potential in studies of inflammatory responses. -
Immunoproteasome/Proteasome Inhibitor
Immunoproteasome inhibitor 1 is a potent reversible inhibitor of the immunoproteasome and the proteasome, targeting the β5c, β1i, and β5i subunits with Kis of 1.18, 0.27, and 1.91 μM, respectively. This compound exhibits significant biological activity in modulating protein degradation pathways, making it a valuable tool for investigating the role of the immunoproteasome in various neoplastic diseases. Its unique mechanism of action facilitates research into targeted therapies and mechanistic studies in oncology. -
Calpain Inhibitor
Ac-Leu-Leu-Norleucinol (ALLN) is a potent calpain inhibitor that plays a critical role in the study of proteolytic pathways. This compound has demonstrated effectiveness in mitigating acetaminophen-induced acute liver damage by lowering the levels of liver enzymes such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Its application extends to research focused on cellular stress responses and the mechanisms of liver injury. -
Ubiquitin-proteasome System Stressor
RAMB4 is a potent ubiquitin-proteasome system (UPS) stressor that inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activities. By triggering a UPS-stress response, RAMB4 effectively disrupts protein homeostasis without directly impacting the catalytic functions of the 20S proteasome. Its unique mechanism positions RAMB4 as a valuable tool for investigating UPS-related pathways and contributes to anticancer research by enhancing cellular stress responses. -
Calpain Inhibitor
(1S,2R)-Alicapistat is a selective inhibitor of human calpains 1 and 2, targeting these proteolytic enzymes involved in cellular signaling. With an IC50 value of 395 nM for calpain 1, it demonstrates significant biological activity, potentially making it valuable in Alzheimer's disease research. This compound's oral bioavailability and specificity may aid in elucidating the role of calpains in neurodegenerative disorders. -
Calpain 1 Inhibitor
Calpain Inhibitor-1 is a selective inhibitor of calpain 1, a cysteine protease, with an IC50 value of 100 nM and a Ki of 2.89 μM. This compound is instrumental in studying calpain-mediated processes, including cellular signaling and apoptosis. It serves as a valuable tool in research applications focusing on neurodegenerative diseases, cardiac protection, and cancer therapy, where calpain activity is implicated.
