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Cathepsin L Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cathepsin (102) Akt (2) Apoptosis (5) Bacterial (1) Beta-secretase (6) Biochemical Assay Reagents (1) Carbonic Anhydrase (1) Casein Kinase (1) Caspase (2) CCR (2) Cytochrome P450 (2) Drug-Linker Conjugates for ADC (1) EGFR (1) Elastase (5) ERK (2) Filovirus (2) Formyl Peptide Receptor (FPR) (1) Glutathione Peroxidase (1) HDAC (1) HSP (1) Interleukin Related (1) Isotope-Labeled Compounds (1) JAK (1) Kallikrein (1) p38 MAPK (2) Parasite (9) Phosphatase (1) Proteasome (7) ROS Kinase (1) SARS-CoV (22) Ser/Thr Protease (5) Src (2) STAT (1) Thrombin (1) Virus Protease (5)
By Research Areas:	Cancer (41) Cardiovascular Disease (3) Infection (33) Inflammation/Immunology (44) Metabolic Disease (13) Neurological Disease (16)
Click Chemistry:	Azide (2) Alkynes (1)

137

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Cathepsin

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-115733

Cathepsin L-IN-2 (Rac)-Z-Phe-Phe-FMK	Cathepsin	Cancer
Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor .

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-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-P4306

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

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-P10117

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

HY-163842

Cathepsin K inhibitor 7	Cathepsin	Inflammation/Immunology
Cathepsin K inhibitor 7 (compound 7) is a Cathepsin K inhibitor with the pK_i of 7.3 aganist CatK. Cathepsin K inhibitor 7 can be used for study of osteoporosis .

HY-P10118

Cathepsin L-IN-3	Cathepsin	Others
Cathepsin L-IN-3 is a tripeptide-sized cathepsin L 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-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-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-105668

Cathepsin S-IN-1	Cathepsin	Others
Cathepsin S-IN-1 (example 1) is a Cathepsin S inhibitor .

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-151524

Cathepsin K inhibitor 3	Cathepsin	Inflammation/Immunology
Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC₅₀ value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies .

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-10042

Odanacatib 5+ 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-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-100231

Cathepsin inhibitor 1	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-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-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-172242

Verducatib	Cathepsin	Cancer
Verducatib is a *cathepsin* inhibitor .

HY-164958

TB-11	Cathepsin Beta-secretase	Cancer
TB-11 is a Cathepsin D inhibitor, with IC₅₀s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research .

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 .

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-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-149926

Cathepsin Inhibitor 3	Ser/Thr Protease	Others
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-103351

Cathepsin G Inhibitor I	Cathepsin	Inflammation/Immunology
Cathepsin G Inhibitor I (compound 7) is an effective, selective, reversible, competitive, non-peptide cathepsin G inhibitor (IC₅₀=53 nM; K_i=63 nM) .

HY-139111

Oxocarbazate	Cathepsin SARS-CoV	Infection
Oxocarbazate is an inhibitor of human cathepsin L with the IC₅₀ values of 6.9 nM (human Cathepsin L,0 h) 0.4 nM ((human Cathepsin L,4 h) and 5.07 μM (human cathepsin B), respectively. Oxocarbazate blockes both SARS-CoV (IC₅₀ = 273 nM) and Ebola virus (IC₅₀ = 193 nM) entry into 293T cells .

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-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-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-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-10042S

Odanacatib-d4 MK-0822-d₄	Isotope-Labeled Compounds	Metabolic Disease Cancer
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 .

HY-P10065

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

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-124202

SQ 32602	Cathepsin	Others
SQ 32602 is an inhibitor of *cathepsin* E, with the IC₅₀ of 88 nM .

HY-P5999

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

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-155611

Cathepsin C-IN-6	Cathepsin	Inflammation/Immunology
Cathepsin C-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsin C with anti-inflammatory activity. Cathepsin C-IN-6 inhibts activation of neutrophil elastase，exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.，chronic obstructive pulmonary disease) .

HY-103350

CA-074 15+ 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-N10109

Gallinamide A	SARS-CoV	Infection
Gallinamide A is a potent inhibitor of cathepsin L with an IC₅₀ value of 17.6 pM.

HY-W796158

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

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-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-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-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-123531

JNJ 10329670	Cathepsin	Inflammation/Immunology
JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a K_i value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation .

HY-15958A

(S,R,R)-VBY-825	Ser/Thr Protease	Cancer
(S,R,R)-VBY-825 is the isomer of VBY-825 (HY-15958), and can be used as an experimental control. VBY-825 is a novel reversible inhibitor of cathepsin with high inhibition of cathepsin B, L, S and V.

Cat. No.	Product Name

HY-L012

Metabolism/Protease Compound Library

5,484 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 5,484 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

Cat. No.	Product Name	Type

HY-W014540

L-Proline tert-butyl ester hydrochloride tert-Butyl L-prolinate hydrochloride	Cell 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-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-P4306

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

HY-P10117

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

HY-P10118

Cathepsin L-IN-3	Cathepsin	Others
Cathepsin L-IN-3 is a tripeptide-sized cathepsin L 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-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-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-W796158

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

HY-P3012

Cathepsin G	Cathepsin	Inflammation/Immunology
Cathepsin G acts as a potent agonist of human platelet activation leading to their aggregation., and can be used for screening of relevant inhibitors .

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-P1081

Acetyl-Calpastatin(184-210)(human)	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-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-141867

Z-FF-FMK Z-Phe-Phe-FMK	Cathepsin	Neurological Disease
Z-FF-FMK is a selective *cathepsin-L* inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .

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-P0111

Z-WEHD-FMK 2 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-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-N4289

3-Epiursolic Acid 1 Publications Verification	Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Rosaceae Plants Disease Research Fields Eriobotrya japonica (Thunb.) Lindl. Cancer	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-N2905

Aurantiamide acetate 1 Publications Verification Asperglaucide	Structural Classification Natural Products Portulacaceae Classification of Application Fields Source classification Portulaca oleracea Linn. Plants Inflammation/Immunology Disease Research Fields	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-N10109A

Gallinamide A TFA	Structural Classification 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) .

HY-16594

Lactacystin 3 Publications Verification	Structural Classification Microorganisms Antibiotics Source classification Other Antibiotics	Proteasome Apoptosis ROS Kinase
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 ^[1] ^[2] ^[3] ^[4] ^[5] ^[6] ^[7] ^[8] ^[9] ^[10].

HY-W744699

Larixol (+)-Larixol	Larix decidua Miller Structural Classification Natural Products Pinaceae Source classification Plants	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-N4288

4-Methylesculetin 1 Publications Verification	Structural Classification Nicotiana tabacum L. Classification of Application Fields Source classification Coumarins Phenols Polyphenols Phenylpropanoids Solanaceae Plants Disease Research Fields 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-N10109

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

HY-N15154

Tasiamide B	Structural Classification 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-129461

Dibenzyl trisulfide DTS	Structural Classification Natural Products Petiveriaceae Source classification Plants Petiveria alliacea	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 .

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-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 .

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Cathepsin L Inhibitor

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Biochemical Assay Reagents

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