Search Result

Pathways Recommended:	Metabolic Enzyme/Protease

Results for "

cathepsin proteases

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cathepsin (22) Ser/Thr Protease (9) Virus Protease (4) Antibiotic (1) Apoptosis (3) Autophagy (2) Bacterial (1) Beta-secretase (2) Biochemical Assay Reagents (1) CCR (2) Cytochrome P450 (2) Elastase (3) Ferroptosis (2) Filovirus (2) Fluorescent Dye (1) HIV (1) HSP (1) Kallikrein (1) Necroptosis (2) Parasite (5) Proteasome (2) Pyroptosis (1) SARS-CoV (9) Thrombin (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (1) Infection (17) Inflammation/Immunology (15) Metabolic Disease (3) Neurological Disease (5)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Targets Recommended: Cathepsin Ser/Thr Protease Proteolytic Enzyme HCV Protease HIV Protease Virus Protease Protease Activated Receptor (PAR)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W790014

Z-FG-NHO-BzOME	Cathepsin	Infection
Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .

HY-Y0241

2-Cyanopyrimidine	Cathepsin	Metabolic Disease
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 .

HY-128971

LHVS	Cathepsin Parasite	Infection Neurological Disease
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 .

HY-158307

Z-Arg-Arg-βNA acetate	Cathepsin	Others
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 .

HY-156655A

Olgotrelvir sodium STI-1558 sodium	SARS-CoV Cathepsin	Infection
Olgotrelvir sodium is an orally active dual inhibitor of *coronavirus main protease* (Mpro)** and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .

HY-E70227

Cathepsin G, human neutrophils CTSH; ACC4; ACC5	Ser/Thr Protease	Inflammation/Immunology
Cathepsin G, human neutrophils (CTSH; ACC4) a serine protease found in polymorphonuclear neutrophils (PMNs), functions in inflammation .

HY-E70226

Cathepsin S, human CTSS	Ser/Thr Protease	Cardiovascular Disease Inflammation/Immunology Cancer
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 .

HY-143714

Cathepsin K inhibitor 2	Cathepsin	Inflammation/Immunology
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) .

HY-149931

BMV109	Fluorescent Dye	Cancer
BMV109 is a quenched probe that becomes fluorescent when cleaved and covalently bound by active cathepsin proteases. BMV109 can be exploited for tumor imaging .

HY-N15154

Tasiamide B	Cathepsin HSP	Cancer
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 .

HY-P5378

Ac-KQKLR-AMC cathepsin S substrate	Ser/Thr Protease	Others
Ac-KQKLR-AMC (Cathepsin S 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 S is a cysteine proteinase involved in the pathogenesis of autoimmune diseases, atherosclerosis, cancer, obesity and related diseases.This peptide is a cathepsin S substrate fluorescently labeled with AMC (Ex/Em=354 nm/442 nm). It can be used to measure cathepsin S activity.)

HY-P5377

Abz-HPGGPQ-EDDnp cathepsin K substrate	Ser/Thr Protease	Others
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.)

HY-100227

E 64c 2 Publications Verification	Cathepsin SARS-CoV	Metabolic Disease
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.

HY-146584

Cathepsin C-IN-5	Cathepsin	Inflammation/Immunology
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 .

HY-P2780

Cathepsin B, Bovine spleen	Apoptosis Ferroptosis Autophagy Necroptosis	Others Cancer
Cathepsin B, Bovine spleen is a cysteine protease and is involved in multiple kinds of programmed cell death (including apoptosis, pyroptosis, ferroptosis, necroptosis, and autophagic cell death) .

HY-18964

MG-101 5+ Cited Publications Calpain inhibitor I; Ac-LLnL-CHO; ALLN	Proteasome Apoptosis	Cancer
MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with K_is 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 .

HY-120288

AM4299B	Cathepsin	Infection Metabolic Disease
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 .

HY-P2780A

Cathepsin B, Human Liver	Apoptosis Cathepsin Pyroptosis Ferroptosis Autophagy Necroptosis	Inflammation/Immunology Cancer
Cathepsin B, Human Liver is a cysteine protease in liver and is involved in multiple kinds of programmed cell death (including apoptosis, pyroptosis, ferroptosis, necroptosis, and autophagic cell death). Cathepsin B (CTSB) have been implicated in various ECM-related disorders, such as dilated cardiomyopathy, lung fibrosis, proteinuric renal disorders, cancer, and osteoporosis .

HY-168599

SARS-CoV-2 Mpro-IN-31	SARS-CoV	Infection
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 .

HY-118355

ALLM Calpain inhibitor II	Proteasome Cathepsin	Neurological Disease
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) .

HY-119293

K777 1 Publications Verification	Cathepsin CCR Cytochrome P450 Parasite SARS-CoV Filovirus	Infection Cancer
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. 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 .

HY-119293A

K777 tosylate	Cathepsin CCR Cytochrome P450 Parasite SARS-CoV Filovirus	Infection Cancer
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 and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. 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 .

HY-168732

MCG-02	Parasite	Infection
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 .

HY-E70228

Cathepsin H, human liver	Ser/Thr Protease	Cancer
Cathepsin H, human liver is an aminopeptidase and an endopeptidase. Involved in the catabolism of proteins in the lysosomal system. Cathepsin H, human liver has a key role in the regulation of the biological behavior of tumor cells and the pathological processes of brain diseases .

HY-W014540

L-Proline tert-butyl ester hydrochloride tert-Butyl L-prolinate hydrochloride	Biochemical Assay Reagents
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.

HY-18234A

Leupeptin hemisulfate Maximum Cited Publications 39 Publications Verification	Cathepsin Ser/Thr Protease Virus Protease	Infection Inflammation/Immunology
Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits M ^pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .

HY-18234

Leupeptin	Ser/Thr Protease Virus Protease Cathepsin	Infection Inflammation/Immunology
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits M ^pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .

HY-126988

SP-Chymostatin B α-MAPI	Elastase	Others
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 .

HY-122523

Tetromycin A	Bacterial	Infection
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.

HY-126489

Tetromycin B	Parasite	Infection
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).

HY-158763

MPI8 TG0205221	SARS-CoV Cathepsin Virus Protease	Infection
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). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .

HY-P4404

Abz-GIVRAK(Dnp)	Cathepsin	Others
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 .

HY-15652

Freselestat ONO-6818; ONO-PO-736	Elastase	Inflammation/Immunology
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a K_i 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 .

HY-167924

Ono 3307 free base	Kallikrein Thrombin Ser/Thr Protease	Inflammation/Immunology
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.

HY-124322

NB-360	Beta-secretase	Neurological Disease Inflammation/Immunology
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC₅₀: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .

HY-144812

Gü1303	Cathepsin	Inflammation/Immunology Cancer
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a K_i of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .

HY-144813

Gü2602	Cathepsin	Inflammation/Immunology Cancer
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a K_i of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen .

HY-15652A

Freselestat quarterhydrate ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate	Elastase	Inflammation/Immunology
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a K_i 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 .

HY-114584

A-953227	Ser/Thr Protease	Neurological Disease
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 .

HY-10472

LY2811376 10+ Cited Publications	Beta-secretase	Neurological Disease
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.

HY-148034

Plm IV inhibitor-1	Others	Infection
Plm IV inhibitor-1 (compound 6) is a potent plasmepsin IV (Plm IV) inhibitor with IC₅₀s of 4.1, 0.80, 0.25, 0.35 µM for Plm I, Plm II, Plm IV, Cat D, respectively .

HY-A0097A

Teicoplanin sodium Antibiotic MDL-507 sodium; MDL-507 sodium	Antibiotic HIV SARS-CoV	Infection
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 .

HY-151900

SARS-CoV-2 Mpro-IN-4	SARS-CoV Virus Protease	Infection
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 .

HY-151901

SARS-CoV-2 Mpro-IN-5	SARS-CoV	Infection
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 .

HY-146581

Cathepsin C-IN-4	Cathepsin	Inflammation/Immunology
Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC₅₀ of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC₅₀ values of 203.4 and 177.6 nM, respectively .

HY-146580

Cathepsin C-IN-3	Cathepsin	Inflammation/Immunology
Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC₅₀ of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC₅₀ values of 101.5 and 86.5 nM, respectively .

Cat. No.	Product Name

HY-L012

Metabolism/Protease Compound Library

5,228 compounds

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 5,228 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

Cat. No.	Product Name	Type