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Results for "

Cathepsin L Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cathepsin (142) Akt (3) Amyloid-β (1) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (14) Bacterial (2) Beta-secretase (8) Biochemical Assay Reagents (1) Carbonic Anhydrase (1) Casein Kinase (1) Caspase (7) Cholecystokinin Receptor (1) Cytochrome P450 (3) Deubiquitinase (2) Dipeptidyl Peptidase (2) DNA/RNA Synthesis (2) Drug-Linker Conjugates for ADC (3) EGFR (1) Elastase (7) Endogenous Metabolite (1) ERK (3) Filovirus (2) Formyl Peptide Receptor (FPR) (1) Glutathione Peroxidase (1) HCV (1) HCV Protease (1) HDAC (2) HSP (1) Interleukin Related (3) Isotope-Labeled Compounds (1) JAK (1) Kallikrein (1) MEK (1) MHC (1) Microtubule/Tubulin (1) MMP (1) NF-κB (1) NO Synthase (1) Nuclear Factor of activated T Cells (NFAT) (1) Ornithine decarboxylase (ODC) (2) p38 MAPK (2) Parasite (10) PARP (1) PD-1/PD-L1 (1) Phosphatase (1) PI3K (1) Proteasome (11) PSMA (1) Raf (1) RANKL/RANK (1) Ras (1) Reactive Oxygen Species (ROS) (3) Reference Standards (13) SARS-CoV (30) Ser/Thr Protease (6) Src (3) STAT (1) Thrombin (1) TNF Receptor (1) Topoisomerase (2) Virus Protease (10) β-glucuronidase (1)
By Research Areas:	Cancer (62) Cardiovascular Disease (7) Infection (43) Inflammation/Immunology (58) Metabolic Disease (23) Neurological Disease (24)
Click Chemistry:	DBCO (1) Azide (2) Alkynes (1)
Oligonucleotides:	Aptamers (1)

187

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

GMP Molecules

Targets Recommended: Cathepsin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100223

Calpeptin 25+ Cited Publications	Cathepsin Proteasome Apoptosis	Inflammation/Immunology
Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID₅₀ of 40 nM for Calpain I in human platelets . Calpeptin is also an inhibitor of cathepsin K .

HY-103350

CA-074 25+ Cited Publications	Cathepsin	Neurological Disease Cancer
CA-074 is a potent inhibitor of cathepsin B with a K_i of 2 to 5 nM.

HY-10042

Odanacatib 10+ Cited Publications MK-0822	Cathepsin	Metabolic Disease Cancer
Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC₅₀ of 0.2 nM for human cathepsin K.

HY-128140

Z-FY-CHO 5+ Cited Publications Z-Phe-Tyr-CHO	Cathepsin	Neurological Disease Metabolic Disease
Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor .

HY-18964

MG-101 10+ 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-119293

K777 3 Publications Verification	Cathepsin Cytochrome P450 Parasite SARS-CoV Filovirus	Infection Inflammation/Immunology 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. 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-103351

Cathepsin G Inhibitor I	Cathepsin	Inflammation/Immunology
Cathepsin G Inhibitor I (Compound 7) is a potent, selective, reversible, competitive, non-peptidic Cathepsin G inhibitor (IC₅₀ = 53 nM; K_i = 63 nM). Cathepsin G Inhibitor I can be used in research related to immune disorders .

HY-114374

RO5461111	Cathepsin	Inflammation/Immunology
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC₅₀s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis .

HY-109069

Petesicatib 1 Publications Verification RO5459072; RG-7625	Cathepsin	Inflammation/Immunology
Petesicatib (RO5459072; RG-7625) is a cathepsin S inhibitor, used in research of immune diseases .

HY-100350

CA-074 methyl ester Maximum Cited Publications 40 Publications Verification CA-074Me	Cathepsin	Neurological Disease Cancer
CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

HY-15100

Balicatib 2 Publications Verification AAE581	Cathepsin	Inflammation/Immunology
Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC₅₀ values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis .

HY-103353

SID 26681509 5 Publications Verification	Cathepsin Parasite	Infection Cancer
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of *human cathepsin* L with an IC₅₀** of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite *Plasmodium falciparum* and inhibits *Leishmania major* with IC₅₀s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .

HY-100231

Cathepsin inhibitor 1 1 Publications Verification	Cathepsin	Inflammation/Immunology
Cathepsin inhibitor 1 (Compound 25) is a potent and selective inhibitor of *Cathepsin, with pIC₅₀s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively. Cathepsin* inhibitor 1 is promising for research of osteoarthritis .

HY-103352

L-006235 L-235	Cathepsin	Metabolic Disease
L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC₅₀ of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (K_i=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (K_i=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .

HY-115733

Cathepsin L-IN-2 1 Publications Verification (Rac)-Z-Phe-Phe-FMK	Cathepsin	Cancer
Cathepsin L-IN-2 ((Rac)-Z-Phe-Phe-FMK) is an isomer of the Cathepsin L inhibitor Z-Phe-Phe-FMK (HY-141867), with an IC₅₀ of 15 μM for cathepsin L. Z-Phe-Phe-FMK irreversibly blocks the proteolytic function of cathepsins by covalently binding to the cysteine residues in the active center of the enzyme. Cathepsin L-IN-2 and Z-Phe-Phe-FMK can be used to study neurodegenerative diseases (such as GRN-related frontotemporal dementia) and cancer invasion and metastasis.

HY-146985

Cathepsin X-IN-1 1 Publications Verification	Cathepsin	Neurological Disease Cancer
Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC₅₀ of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic .

HY-102087

JPM-OEt 3 Publications Verification	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .

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-N4289

3-Epiursolic Acid 1 Publications Verification	Cathepsin	Cancer
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC₅₀, 6.5 μM; K_i, 19.5 μM), with no obvious effect on cathepsin B .

HY-15958

VBY-825 1 Publications Verification	Cathepsin	Inflammation/Immunology Cancer
VBY-825 is an orally available novel reversible *cathepsin* inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects .

HY-156655A

Olgotrelvir sodium STI-1558 sodium	SARS-CoV Cathepsin Virus Protease	Infection
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 .

HY-10294

Relacatib SB-462795	Cathepsin	Metabolic Disease Cancer
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with K_i values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC₅₀ values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .

HY-118355

ALLM 1 Publications Verification 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-136888

MeOSuc-AAPV-CMK Elastase Inhibitor III	Elastase Cathepsin	Others
MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .

HY-P4306

Z-Phe-Phe-Diazomethylketone	Cathepsin	Inflammation/Immunology
Z-Phe-Phe-Diazomethylketone is a selective inhibitor of *cathepsin* L .

HY-112318A

GSK-2793660	Cathepsin	Inflammation/Immunology
GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis .

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-152204

Cathepsin L/S-IN-1	Cathepsin	Cancer
Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC₅₀s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells .

HY-W796158

Z-DEVD-CMK	Cathepsin	Inflammation/Immunology
Z-DEVD-CMK is an irreversible inhibitor of most of the *cathepsins* in vitro .

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-148298

CatD-IN-1	Cathepsin	Inflammation/Immunology
CatD-IN-1 (Compound 5) is a Cathepsin D inhibitor with an IC₅₀ of 0.44 μM. CatD-IN-1 holds potential for research in the field of osteoarthritis .

HY-108044

ONO-5334	Cathepsin SARS-CoV	Metabolic Disease
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with K_i values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC₅₀ value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease .

HY-137392

Cathepsin L-IN-4 1-Naphthalenesulfonyl-Ile-Trp-CHO	Cathepsin	Others
Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC₅₀ at nanomolar concentrations .

HY-U00377

Cathepsin Inhibitor 2	Cathepsin	Inflammation/Immunology Cancer
Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a K_i of <20 nM.

HY-147774

Cathepsin K inhibitor 6	Cathepsin	Others
Cathepsin K inhibitor 6 (compound 19) is an inhibitor of cathepsin K (Cat K) with an IC₅₀ of 17 nM. Cathepsin K inhibitor 6 also has inhibitory effects on other isoforms, with IC₅₀s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively .

HY-164634

CLIK-148	Cathepsin Cholecystokinin Receptor	Neurological Disease Metabolic Disease Cancer
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 .

HY-170772

Dual Cathepsin L/JAK-IN-1	p38 MAPK STAT Interleukin Related Cathepsin JAK	Inflammation/Immunology
Dual Cathepsin L/JAK-IN-1 (Compound A8) is a dual inhibitor of Cathepsin L (CTSL) and JAK, with IC₅₀ values of 0.68 μM, 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for CTSL, JAK1/2/3, and TYK2, respectively. Dual Cathepsin L/JAK-IN-1 effectively blocks the activation of the MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. Dual Cathepsin L/JAK-IN-1 can be used in research on acute lung injury (ALI) .

HY-156655

Olgotrelvir STI-1558	SARS-CoV Virus Protease Cathepsin	Infection
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 .

HY-115454A

GB111-NH2 hydrochloride	Cathepsin	Others
GB111-NH2 hydrochloride is a cysteine cathepsin inhibitor, and can be used for cancer study .

HY-112318

GSK-2793660 free base	Cathepsin	Inflammation/Immunology
GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis .

HY-50887

L-873724	Cathepsin	Metabolic Disease
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC₅₀s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively . L-873724 also exhibits an IC₅₀ of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption .

HY-177315

Cathepsin K-IN-8	Cathepsin	Inflammation/Immunology Cancer
Cathepsin K-IN-8 (cxample 6-60) is a cathepsin K inhibitor that can be used for the study of inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors .

HY-112583

MIV-247	Cathepsin	Neurological Disease
MIV-247 is a selective cathepsin S inhibitor with K_is of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.

HY-164956

TB-9	Cathepsin Beta-secretase	Cancer
TB-9, a Tasiamide B (HY-N15154) derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC₅₀s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively .

HY-174380

DPP-1-IN-1	Dipeptidyl Peptidase Ser/Thr Protease Elastase	Inflammation/Immunology
DPP-1-IN-1 (Compound 14) is an orally active inhibitor of Cathepsin C (also known as Dipeptidyl peptidase I) with an IC₅₀ of 5.31 nM. DPP-1-IN-1 can inhibit the activity of Cathepsin C downstream Neutrophil elastase in neutrophils. DPP-1-IN-1 can be used in the research of inflammatory diseases .

HY-119293A

K777 tosylate	Cathepsin Cytochrome P450 Parasite SARS-CoV Filovirus	Infection Inflammation/Immunology 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. 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-169171

Cathepsin L-IN-5	Cathepsin	Infection
Cathepsin L-IN-5 (D6-3) is a potent Cathepsin L (CatL) inhibitor with an IC₅₀ of 0.27 nM. Cathepsin L-IN-5 effectively blocks the CatL function and substantially hinders the entry of the SARS-CoV-2 pseudovirus to cells by inhibiting the cleavage of the spike protein. Cathepsin L-IN-5 can be utilized in SARS-CoV-2 research .

HY-161721

Cathepsin Inhibitor 4	Cathepsin	Cancer
Cathepsin Inhibitor 4 (Compound 45) is a selective inhibitor for Cathepsin S with K_i of 0.04 nM .

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-P10118A

Cathepsin L-IN-3 TFA	Cathepsin	Others
Cathepsin L-IN-3 (Compound cat L inh. 7) TFA is selective a noncovalent cathepsin L inhibitor with a K_i of 4.3 nM .

Cat. No.	Product Name

HY-L012

Metabolism/Protease Compound Library

7,056 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 7,056 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

Cat. No.	Product Name	Type

HY-164729

FZ-AD005

Fluorescent Dyes

FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The K_d value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .

HY-18964G

MG-101

Calpain Inhibitor I; Ac-LLnL-CHO; ALLN

Fluorescent Dyes

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 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 .

Cat. No.	Product Name	Type

HY-18964G

MG-101

Calpain Inhibitor I; Ac-LLnL-CHO; ALLN

Biochemical Assay Reagents

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-W745090

Isomaltulose monohydrate

Biochemical Assay Reagents

Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .

Cat. No.	Product Name	Target	Research Area

HY-P0111

Z-WEHD-FMK 4 Publications Verification Z-WE(OMe)HD(OMe)-FMK	Caspase Cathepsin	Cancer
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC₅₀=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .

HY-136888

MeOSuc-AAPV-CMK Elastase Inhibitor III	Elastase Cathepsin	Others
MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .

HY-141867

Z-FF-FMK Z-Phe-Phe-FMK	Cathepsin MEK Caspase DNA/RNA Synthesis Apoptosis	Cardiovascular Disease Neurological Disease
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 .

HY-P4306

Z-Phe-Phe-Diazomethylketone	Cathepsin	Inflammation/Immunology
Z-Phe-Phe-Diazomethylketone is a selective inhibitor of *cathepsin* L .

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-W796158

Z-DEVD-CMK	Cathepsin	Inflammation/Immunology
Z-DEVD-CMK is an irreversible inhibitor of most of the *cathepsins* in vitro .

HY-P1081

Acetyl-Calpastatin(184-210)(human) 1 Publications Verification	Proteasome	Inflammation/Immunology
Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with K_i values of 0.2 nM and 6 μM for μ-calpain and cathepsin L, respectively .

HY-137392

Cathepsin L-IN-4 1-Naphthalenesulfonyl-Ile-Trp-CHO	Cathepsin	Others
Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC₅₀ at nanomolar concentrations .

HY-P4532

Ac-Leu-Val-Lys-Aldehyde	Cathepsin	Neurological Disease
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC₅₀s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II .

HY-P5898

Z-Val-Val-Nle-diazomethylketone Z-Val-Val-Nle-CHN2	Cathepsin MHC	Inflammation/Immunology
Z-Val-Val-Nle-diazomethylketone is a cathepsin S (CATS) inhibitor. Z-Val-Val-Nle-diazomethylketone significantly inhibits the IFNg-induced upregulation of the MHCII molecules HLA-DR and Ii-p33/35 with an increase of Ii-p10 protein level. Z-Val-Val-Nle-diazomethylketone can be used for dermatological diseases like psoriasis, atopic dermatitis and actinic keratosis research .

HY-P10118A

Cathepsin L-IN-3 TFA	Cathepsin	Others
Cathepsin L-IN-3 (Compound cat L inh. 7) TFA is selective a noncovalent cathepsin L inhibitor with a K_i of 4.3 nM .

HY-P10117

Cathepsin K inhibitor 5	Cathepsin	Metabolic Disease
Cathepsin K inhibitor 5 is a potent Cathepsin K inhibitor .

HY-P10061

Cathepsin K inhibitor 4	Cathepsin	Cancer
Cathepsin K inhibitor 4 is a potent carbohydrazide Cathepsin K inhibitor with IC₅₀s of 13 nM, 269 nM, 296 nM for human, rat, mouse Cathepsin K, respectively .

HY-P10118

Cathepsin L-IN-3	Cathepsin	Others
Cathepsin L-IN-3 (Compound cat L inh. 7) is selective a noncovalent cathepsin L inhibitor with a K_i of 4.3 nM .

HY-P10065

RKLLW-NH2	Cathepsin	Inflammation/Immunology
RKLLW-NH2 is a Cathepsin L inhibitor .

HY-P5999

Z-FG-NHO-Bz	Cathepsin	Cancer
Z-FG-NHO-Bz is a selective *cathepsin* inhibitor .

HY-P1081A

Acetyl-Calpastatin(184-210)(human) TFA	Proteasome	Inflammation/Immunology
Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with K_i values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively .

HY-P0109

(S,S)-Z-FA-FMK	Cathepsin	Others
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-16594

Lactacystin Maximum Cited Publications 8 Publications Verification	Structural Classification Microorganisms Antibiotics Other Antibiotics Source Classification	Proteasome Cathepsin Apoptosis
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC₅₀ = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on ^[2] ^[6] .

HY-N2905

Aurantiamide acetate 3 Publications Verification Asperglaucide	Natural Products Portulacaceae Classification of Application Fields Portulaca oleracea Linn. Plants Inflammation/Immunology Disease Research Fields Source Classification	Cathepsin
Aurantiamide acetate (TMC-58A) is a selective and orally active *cathepsin* inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases .

HY-N4288

4-Methylesculetin 3 Publications Verification	Structural Classification Nicotiana tabacum L. Classification of Application Fields Coumarins Phenols Polyphenols Phenylpropanoids Solanaceae Plants Disease Research Fields Source Classification Cancer	Glutathione Peroxidase Cathepsin Phosphatase
4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases .

HY-N6037

Gardenin B	Monophenols Flavonoids Classification of Application Fields Flavones Rubiaceae Phenols Plants Gardenia jasminoides Ellis Disease Research Fields Source Classification Cancer	Apoptosis Deubiquitinase Ornithine decarboxylase (ODC) Cathepsin Reactive Oxygen Species (ROS) Caspase
Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC₅₀: 6.24 μg/mL), and Cathepsin D (IC₅₀: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC₅₀ values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research .

HY-N4289

3-Epiursolic Acid 1 Publications Verification	Triterpenes Classification of Application Fields Terpenoids Rosaceae Plants Disease Research Fields Eriobotrya japonica (Thunb.) Lindl. Cancer Source Classification	Cathepsin
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC₅₀, 6.5 μM; K_i, 19.5 μM), with no obvious effect on cathepsin B .

HY-129461

Dibenzyl trisulfide DTS	Natural Products Petiveriaceae Plants Petiveria alliacea Source Classification	Cathepsin
Dibenzyl trisulfide (DTS) is an active ingredient that can be isolated from Petiveria alliacea L.. Dibenzyl trisulfide inhibits cell proliferation and migration. Dibenzyl trisulfide decreased the mRNA and protein expression of BAK-1 and LTA. Dibenzyl trisulfide induces lysosomal membrane permeabilization and cathepsin B release .

HY-N15154

Tasiamide B	Natural Products Marine algae Marine natural products Source Classification	Cathepsin HSP
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-W744699

Larixol (+)-Larixol	Larix decidua Miller Natural Products Pinaceae Plants Source Classification	Src ERK Akt
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM), cathepsin G release (IC₅₀: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .

HY-N6037R

Gardenin B (Standard)	Structural Classification Monophenols Flavonoids Flavones Rubiaceae Phenols Plants Gardenia jasminoides Ellis Source Classification	Reference Standards Apoptosis Ornithine decarboxylase (ODC) Reactive Oxygen Species (ROS) Cathepsin Deubiquitinase Caspase
Gardenin B (Standard) is the analytical standard of Gardenin B (HY-N6037). This product is intended for research and analytical applications. Gardenin B is a flavonoid isolated from Gardenia jasminoides. Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC₅₀: 6.24 μg/mL), and Cathepsin D (IC₅₀: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC₅₀ values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research .

HY-N10109

Gallinamide A	Infection Natural Products Microorganisms Classification of Application Fields Disease Research Fields Source Classification	SARS-CoV
Gallinamide A is a potent inhibitor of cathepsin L with an IC₅₀ value of 17.6 pM.

HY-N10109A

Gallinamide A TFA	Natural Products Microorganisms Source Classification	SARS-CoV Parasite Cathepsin
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC₅₀: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC₅₀: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC₅₀: 50 nM) .

Cat. No.	Product Name	Chemical Structure

HY-10042S

Odanacatib-d4
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsin K, with an IC₅₀ of 0.2 nM for human cathepsin K .

Cat. No.	Product Name		Classification

HY-131158

DBCO-PEG3-Glu-VC-PABC-MMAF		DBCO
DBCO-PEG3-Glu-VC-PABC-MMAF (compound s19b) is a drug-linker conjugate for ADC by using the tubulin inhibitor, MMAF (HY-15579), linked via cathepsin cleavable DBCO-PEG3-Glu-VC-PABC. DBCO-PEG3-Glu-VC-PABC-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs) .

HY-149926

Cathepsin Inhibitor 3		Alkynes
Cathepsin Inhibitor 3 (Compound 53k) is a non-radioactive intermediate in compound [ ¹⁸F] 2k radioactive synthesis, which has selectivity for cathepsin S. Cathepsin Inhibitor 3 can undergo radioactive fluorination and can be used for fluorine-18 labeling research . Cathepsin Inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-159128

hCAIX-IN-21		Azide
hCAIX-IN-21 (compound 16c) is a potent hCAIX inhibitor with K_I values of 5.2, 3.5, 12.6, 13600 nM for hCAIX, hCA II, hCA XII, hCA I, respectively. hCAIX-IN-21 inhibits cathepsin B enzyme activity .

HY-159129

hCAXII-IN-10		Azide
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a K_i value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .

Cat. No.	Product Name		Classification

HY-177571

Sgc8c-M Sgc8c-VcMMAE		Aptamers
Sgc8c-M is a PTK7-targeted aptamer-drug conjugate (ApDC). Sgc8c-M is composed of the classic PTK7-specific aptamer Sgc8c, a cathepsin B (CTSB)-cleavable valine-citrulline (VC)-based linker, and the potent antimitotic agent Monomethyl auristatin E (MMAE) (HY-15162) as the payload. Sgc8c-M inhibits the growth of PTK7-overexpressing cancer cells. Sgc8c-M can be used for the study of PTK7-expressing advanced solid tumors .

Targets Recommended: Cathepsin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18964G

MG-101 Calpain Inhibitor I; Ac-LLnL-CHO; ALLN	Proteasome Apoptosis	Cancer
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 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 .

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Cathepsin L Inhibitor

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