Search Result
Results for "
cathepsin L protease
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-18964
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MG-101
Maximum Cited Publications
13 Publications Verification
Calpain inhibitor I; Ac-LLnL-CHO; ALLN
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Proteasome
Apoptosis
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Cancer
|
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MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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- HY-119293
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K777
3 Publications Verification
|
Cathepsin
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Inflammation/Immunology
Cancer
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K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
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- HY-P2780
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-
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- HY-128971
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LHVS
3 Publications Verification
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Cathepsin
Parasite
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Infection
Neurological Disease
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LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM .
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- HY-10472
-
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Beta-secretase
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Neurological Disease
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LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
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- HY-142021
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Cathepsin
Parasite
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Infection
Inflammation/Immunology
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Z-Leu-Arg-AMC is a fluorogenic peptide substrate for cysteine proteases (e.g., Cathepsin) (Ex=350 nm,Em=460 nm). Z-Leu-Arg-AMC is preferentially cleaved by Cathepsin K and S under weakly acidic conditions, while its hydrolysis relies on residual Cathepsin S activity at neutral pH. Z-Leu-Arg-AMC serves as a substrate for recombinant Sphenophorus levis Cathepsin L, falcipain-2, falcipain-3, berghepain-2, knowlepain-2, vivapain-2, as well as falcipain-2 chimeras and constructs. It enables quantitative detection of cysteine protease activity in human inflammatory bronchoalveolar lavage fluid via fluorescence generation. Z-Leu-Arg-AMC can be used in research related to pulmonary inflammatory diseases and malaria .
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- HY-15652
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ONO-6818; ONO-PO-736
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Elastase
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Inflammation/Immunology
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Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
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- HY-100227
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E 64c
3 Publications Verification
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Cathepsin
SARS-CoV
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Metabolic Disease
|
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E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
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- HY-146584
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|
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Cathepsin
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Inflammation/Immunology
|
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Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity .
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- HY-149931
-
|
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Fluorescent Dye
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Cancer
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BMV109 is a quenched probe that becomes fluorescent when cleaved and covalently bound by active cathepsin proteases. BMV109 can be exploited for tumor imaging .
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- HY-156655A
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STI-1558 sodium
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SARS-CoV
Cathepsin
Virus Protease
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Infection
|
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Olgotrelvir (STI-1558) sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
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- HY-118355
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ALLM
1 Publications Verification
Calpain inhibitor II
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Proteasome
Cathepsin
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Neurological Disease
|
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ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI) .
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- HY-P4425
-
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Biochemical Assay Reagents
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Others
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Gly-Phe-AMC is a fluorogenic peptide substrate consisting of a peptide sequence composed of glycine and phenylalanine, linked to the fluorophore AMC. Gly-Phe-AMC also serves as a cathepsin C substrate. Gly-Phe-AMC is widely used to detect the activity of various proteases .
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- HY-141867
-
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Z-Phe-Phe-FMK
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Cathepsin
MEK
Caspase
DNA/RNA Synthesis
Apoptosis
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Cardiovascular Disease
Neurological Disease
|
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Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
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- HY-10242
-
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BILN 2061; BILN 2061ZW
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HCV
HCV Protease
DNA/RNA Synthesis
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Infection
|
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Ciluprevir (BILN 2061; BILN 2061ZW) is an orally active macrocyclic peptide inhibitor of hepatitis C virus (HCV)NS3 protease, with an IC50 of 3 nM. Ciluprevir has Kᵢ values of 0.66 nM and 0.30 nM against genotypes 1b and 1a, respectively. Ciluprevir inhibits HCV RNA replication with an EC50 of 1.2 nM, and its EC50 values against genotypes 1b and 1a are 3 nM and 4 nM, respectively. Ciluprevir shows no significant inhibition against human leukocyte elastase and hepatic cathepsin B. Ciluprevir can be used for genotype 1 HCV infection .
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- HY-W790014
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Cathepsin
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Infection
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Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .
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- HY-E70226
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CTSS
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Ser/Thr Protease
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Cathepsin S, human, is a potent cysteine protease that promotes the degradation of damaged or harmful proteins in the endolysosomal pathway. Cathepsin S, human, is involved in multiple pathological processes, including arthritis, cancer, and cardiovascular disease .
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- HY-P3012
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Cathepsin
ERK
p38 MAPK
PKC
Protease Activated Receptor (PAR)
MMP
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Inflammation/Immunology
|
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Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases .
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- HY-42709
-
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Carbobenzoxy-L-valyl-L-alanine
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Amino Acid Derivatives
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Cancer
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Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsin B and other lysosomal proteases to enable payload release following lysosomal internalization. Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
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- HY-172242
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Cathepsin
Dipeptidyl Peptidase
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Inflammation/Immunology
|
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Verducatib (BI 1291583) is an orally active inhibitor of cathepsin C (also known as DPP1). Verducatib restores the protease-inhibitor balance by inhibiting the activation of neutrophil serine proteases, thereby alleviating pulmonary inflammation and regulating infection responses. Verducatib significantly reduces the risk (including severe exacerbations) and frequency of acute exacerbations in bronchiectasis (BE). Verducatib also improves lung function and quality of life, and shortens the duration of antibiotic use. The overall incidence of adverse events of Verducatib is comparable to that of placebo, with only slightly more mild-to-moderate cutaneous adverse events observed in the high-dose group, demonstrating promising clinical application potential .
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- HY-P2922
-
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Cathepsin
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Cancer
|
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Cathepsin C is a lysosomal cysteine protease essential for catalytic activation of many serine proteases, including proteinase 3 (PR3), neutrophil elastase (NE), cathepsin G (CTSG), granzyme A/B/C, and mast cell chymase .
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- HY-P3153
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Cathepsin
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Metabolic Disease
|
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Cathepsin K is a cysteine protease with endo and collagenolytic activities. Cathepsin K induces degradation of bone collagen and can be used for the research of osteoporosis .
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- HY-Y0241
-
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Cathepsin
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Metabolic Disease
|
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2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos .
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- HY-N6674
-
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ECO-4601; TLN-4601; BU 4664L
|
Apoptosis
Bacterial
Cathepsin
Parasite
Endogenous Metabolite
|
Infection
Inflammation/Immunology
Cancer
|
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Diazepinomicin (ECO-4601) is an anticancer and antibacterial agent. Diazepinomicin can be produced by a Micromonospora strain. Diazepinomicin induces Apoptosis. Diazepinomicin inhibits the proteases Rhodesain and Cathepsin L at an IC50 of 70-90 μM. Diazepinomicin possesses anti-inflammatory and anti-tumor activity. Diazepinomicin has demonstrated activity against hepatocellular carcinoma. Diazepinomicin shows antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 μM. Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL .
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- HY-P2750
-
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CTSD
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Biochemical Assay Reagents
|
Cardiovascular Disease
Neurological Disease
Cancer
|
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Cathepsin D (CTSD) is a lysosomal aspartic protease encoded by the CTSD gene. Cathepsin D regulates lysosomal protease activity. Loss of Cathepsin D leads to lysosomal dysfunction and the accumulation of various cellular proteins associated with neurodegenerative diseases. Cathepsin D is involved in breast cancer metastasis. Cathepsin D can be used in research on diseases such as breast cancer and stroke .
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- HY-158307
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Cathepsin
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Others
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Z-Arg-Arg-βNA acetate is a sensitive dipeptide substrate of the protease Cathepsin B and resistant to proteases H and L. Z-Arg-Arg-βNA acetate can serve as an important tool for distinguishing non-Cathepsin B type proteins .
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- HY-156655
-
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STI-1558
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SARS-CoV
Virus Protease
Cathepsin
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Infection
|
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Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
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- HY-164634
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Cathepsin
Cholecystokinin Receptor
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Neurological Disease
Metabolic Disease
Cancer
|
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CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing .
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- HY-119293A
-
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Cathepsin
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Inflammation/Immunology
Cancer
|
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K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
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- HY-N15154
-
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Cathepsin
HSP
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Cancer
|
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Tasiamide B is a Cathepsin D inhibitor, which is a linear peptide found in the marine cyanobacteria Symploca sp.. Tasiamide B is proved as a good template for the development of aspartic proteases inhibitors. Tasiamide B is effective against skin cancer by strongly interacting with the target protein HSP90 .
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- HY-A0097A
-
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Antibiotic MDL-507 sodium; MDL-507 sodium
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Antibiotic
HIV
SARS-CoV
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Infection
|
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Teicoplanin sodium is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity .
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- HY-143714
-
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Cathepsin
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Inflammation/Immunology
|
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Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78) .
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- HY-P5377
-
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cathepsin K substrate
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Ser/Thr Protease
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Others
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Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
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- HY-176229
-
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SARS-CoV
Cathepsin
Virus Protease
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Infection
|
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Mpro/Cathepsin L-IN-2 (Compound 1) is a dual irreversible inhibitor of SARS-CoV-2 main protease (M pro, pIC50=8.61) and human cathepsin L (hCTSL, pIC50=7.64). Mpro/Cathepsin L-IN-2 is promising for research of COVID-19 and other coronavirus infections .
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- HY-158763
-
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TG0205221
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
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MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 can be used in clinical studies of COVID-19 .
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- HY-158763A
-
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TG0205221 TFA
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
|
MPI8 (TG0205221) TFA is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 TFA exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 TFA can be used in clinical studies of COVID-19 .
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- HY-106058
-
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Cathepsin
Apoptosis
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Cardiovascular Disease
Cancer
|
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NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors .
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- HY-18964G
-
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Calpain inhibitor I; Ac-LLnL-CHO; ALLN
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Proteasome
Apoptosis
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Cancer
|
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MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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- HY-15652A
-
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ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
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Elastase
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Inflammation/Immunology
|
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Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
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- HY-172977
-
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Cathepsin
NO Synthase
TNF Receptor
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Neurological Disease
Inflammation/Immunology
|
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FGA139 is a cysteine proteases inhibitor with IC50 values of 4.98/3.14 μM for cathepsin B/L. FGA139 reduces LPS-induced NO production in RAW264.7 cells and tumor necrosis factor (TNFα) levels in microglia, and has anti-oxidative stress and anti-inflammatory activities. FGA139 promotes the secretion of neuroprotective metabolites purine and linoleic acid by LPS-stimulated microglia. FGA139 can be used in neuroinflammatory diseases research .
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- HY-123185
-
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Cathepsin
Caspase
SARS-CoV
Interleukin Related
NF-κB
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Infection
|
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(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages .
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- HY-171045
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-
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- HY-120288
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Cathepsin
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Infection
Metabolic Disease
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AM4299B is an inhibitor for thiol protease. AM4299B inhibits bovine spleen cathepsin B, human kidney cathepsin L and papain with IC50s of 0.7, 0.5 and 20 μM, respectively. AM4299B can be used in research in osteoporosis, and has potential to be used as an antiparasitic agent .
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- HY-168599
-
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SARS-CoV
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Infection
|
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SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 M Pro with an IC50 value of 11 nM. Additionally, SARS-CoV-2 Mpro-IN-31 effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively .
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- HY-W014540
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tert-Butyl L-prolinate hydrochloride
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Biochemical Assay Reagents
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L-Proline tert-butyl ester hydrochloride (tert-Butyl L-prolinate hydrochloride) is a biologically active compound that has the activity of inhibiting cysteine and cathepsins, and is therefore widely used in the research and development of protease inhibitors. The characteristics of L-Proline tert-butyl ester hydrochloride make it of great significance in the field of biochemistry.
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-
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- HY-126988
-
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α-MAPI
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Elastase
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Others
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SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .
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- HY-126489
-
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Parasite
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Infection
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Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsin B, respectively. It inhibits the growth of T. brucei in vitro (IC50=30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC50s=71.77 and 20.2 μM, respectively).
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- HY-122523
-
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Bacterial
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Infection
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Tetromycin A is a tetronic acid-based antibiotic. It reportedly has pronounced activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Related tetromycin derivatives have been found to have anti-trypanosomal activity and inhibit the cysteine protease cathepsin L with Ki values in the low micromolar range.
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- HY-P4404
-
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Cathepsin
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Others
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Abz-GIVRAK(Dnp) is the most efficient substrate for cathepsin B and is highly selective for this enzyme among lysosomal cysteine proteases. After Abz-GIVRAK(Dnp) is hydrolyzed, aminoacylbenziminosulfosuccinic acid (Abz-SAS) is released, and dinitrobenzoyl (Dnp) is also released. The product of this hydrolysis reaction, Abz-SAS, is fluorescent under ultraviolet light and can emit a fluorescent signal .
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- HY-114584
-
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Ser/Thr Protease
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Neurological Disease
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A-953227 is a highly potent and selective inhibitor with the activity of inhibiting calcium-dependent esterase (calpain). A-953227 has enhanced selectivity for related cysteine proteases (cathepsins) and has shown good efficacy in cell experiments. A-953227 has shown broad efficacy in preclinical models for Alzheimer's disease, suggesting that it has potential benefits in inhibiting Alzheimer's disease .
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- HY-151901
-
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SARS-CoV
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Infection
|
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SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM .
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- HY-151900
-
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SARS-CoV
Virus Protease
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Infection
|
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SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM .
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- HY-167924
-
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Kallikrein
Thrombin
Ser/Thr Protease
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Inflammation/Immunology
|
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Ono 3307 Free base is a novel synthetic protease inhibitor that exhibits protective effects against acute pancreatitis by preventing hyperamylasemia and pancreatic edema. Ono 3307 Free base also inhibits the redistribution of lysosomal enzymes in acinar cells and mitigates lactic dehydrogenase discharge. Ono 3307 Free base effectively reduces cathepsin B leakage from lysosomes in a dose-dependent manner. Ono 3307 Free base is able to target trypsin (Ki=48 nM), thrombin (Ki=0.18 μM), plasma kallikrein (Ki=0.29 μM), plasmin (Ki=0.31 μM), pancreatic kallikrein (Ki=3.6 μM), and chymotrypsin (Ki=47 μM).
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- HY-183940
-
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Cathepsin
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Infection
Cancer
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Cathepsin L-IN-7 is an inhibitor of cathepsin L, cathepsin B and cathepsin S. Cathepsin L-IN-7 has an IC50 of 0.011 μM against cathepsin L and an IC50 of 0.062 μM against cathepsin S, while it shows weak inhibitory activity against cathepsin B. Cathepsin L-IN-7 binds to the active site of cysteine proteases and blocks their proteolytic function. Cathepsin L-IN-7 can be used in research on viral infections and cancer .
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- HY-Y0241R
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- HY-181513
-
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Interleukin Related
TNF Receptor
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Inflammation/Immunology
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DPP-1-IN-2 is a DPP-I inhibitor with a human IC50 of 36.8 nM and oral efficacy. DPP-1-IN-2 binds to intracellular DPP-I, increases its thermal stability, and reduces the activity and expression levels of downstream neutrophil serine proteases by inhibiting its enzymatic activity. DPP-1-IN-2 regulates the secretion of inflammatory factors and chemokines to exert anti-inflammatory effects. DPP-1-IN-2 reverses joint inflammation and tissue damage in adjuvant-induced arthritis rat models. DPP-1-IN-2 is applicable to research related to arthritis .
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- HY-168732
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Parasite
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Infection
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MCG-02 is the inhibitor for cruzain (CRZ) and cathepsin L-like protease (CATL), that inhibits the CRZ in Trypanosoma cruzi and CATL in Trypanosoma brucei with the IC50 0.2 μM and 0.02 μM .
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- HY-180229
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SARS-CoV
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Infection
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GK730 is a potent and selective SARS-CoV-2 main protease inhibitor with an IC50 of 5.75 nM. GK730 does not inhibit cathepsin B, while exhibits weak inhibition of cathepsin L (IC50 = 11 μM). GK730 can simultaneously block the replication of the virus and the entry pathways for variants such as Omicron into cells. GK730 demonstrates an EC50 value of 5.70 μM against a wild-type SARS-CoV-2 strain in Vero E6 cells and CC50 value greater than 100 μM. GK730 can be used for the research of COVID-19 .
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- HY-10472R
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Reference Standards
Beta-secretase
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Neurological Disease
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LY2811376 (Standard) is the analytical standard of LY2811376 (HY-10472). This product is intended for research and analytical applications. LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
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- HY-179612
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SARS-CoV
Cathepsin
Proteasome
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Infection
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SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL pro protease (b. SARS-CoV-2 3CL pro protease) with an IC50 of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL pro protein of SARS-CoV-1, with its IC50 being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC50 being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection .
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HY-L012
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7,056 compounds
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Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.
MCE designs a unique collection of 7,056 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.
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- HY-18964G
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Calpain inhibitor I; Ac-LLnL-CHO; ALLN
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Fluorescent Dyes
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MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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- HY-18964G
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Calpain inhibitor I; Ac-LLnL-CHO; ALLN
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Biochemical Assay Reagents
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MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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- HY-W014540
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tert-Butyl L-prolinate hydrochloride
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Biochemical Assay Reagents
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L-Proline tert-butyl ester hydrochloride (tert-Butyl L-prolinate hydrochloride) is a biologically active compound that has the activity of inhibiting cysteine and cathepsins, and is therefore widely used in the research and development of protease inhibitors. The characteristics of L-Proline tert-butyl ester hydrochloride make it of great significance in the field of biochemistry.
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| Cat. No. |
상품명 |
Target |
Research Area |
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- HY-P4425
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Biochemical Assay Reagents
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Others
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Gly-Phe-AMC is a fluorogenic peptide substrate consisting of a peptide sequence composed of glycine and phenylalanine, linked to the fluorophore AMC. Gly-Phe-AMC also serves as a cathepsin C substrate. Gly-Phe-AMC is widely used to detect the activity of various proteases .
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- HY-141867
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Z-Phe-Phe-FMK
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Cathepsin
MEK
Caspase
DNA/RNA Synthesis
Apoptosis
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Cardiovascular Disease
Neurological Disease
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Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
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- HY-W790014
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Cathepsin
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Infection
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Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .
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- HY-P3012
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Cathepsin
ERK
p38 MAPK
PKC
Protease Activated Receptor (PAR)
MMP
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Inflammation/Immunology
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Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases .
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- HY-42709
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Carbobenzoxy-L-valyl-L-alanine
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Amino Acid Derivatives
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Cancer
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Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsin B and other lysosomal proteases to enable payload release following lysosomal internalization. Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
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- HY-158307
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Cathepsin
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Others
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Z-Arg-Arg-βNA acetate is a sensitive dipeptide substrate of the protease Cathepsin B and resistant to proteases H and L. Z-Arg-Arg-βNA acetate can serve as an important tool for distinguishing non-Cathepsin B type proteins .
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- HY-P5377
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cathepsin K substrate
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Ser/Thr Protease
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Others
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Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
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- HY-P4404
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Cathepsin
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Others
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Abz-GIVRAK(Dnp) is the most efficient substrate for cathepsin B and is highly selective for this enzyme among lysosomal cysteine proteases. After Abz-GIVRAK(Dnp) is hydrolyzed, aminoacylbenziminosulfosuccinic acid (Abz-SAS) is released, and dinitrobenzoyl (Dnp) is also released. The product of this hydrolysis reaction, Abz-SAS, is fluorescent under ultraviolet light and can emit a fluorescent signal .
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| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-18964G
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Calpain inhibitor I; Ac-LLnL-CHO; ALLN
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Proteasome
Apoptosis
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Cancer
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MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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