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Results for "

protease

" in MCE Product Catalog:

212

Inhibitors & Agonists

3

Screening Libraries

2

Dye Reagents

4

Biochemical Assay Reagents

36

Peptides

2

MCE Kits

24

Natural
Products

58

Recombinant Proteins

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-108717
    Protease K

    Others Others
    Protease K is a nonspecific serine protease that is useful for general digestion of proteins. Protease K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures.
  • HY-P0283
    Protease-Activated Receptor-2, amide

    Protease-Activated Receptor (PAR) Cancer
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
  • HY-P0297
    Protease-Activated Receptor-4

    Protease-Activated Receptor (PAR) Others
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
  • HY-P1308
    SLIGRL-NH2

    protease-Activated Receptor-2 Activating Peptide

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-P1308A
    SLIGRL-NH2 TFA

    protease-Activated Receptor-2 Activating Peptide TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-P2518
    Protease-Activated Receptor-1, PAR-1 Agonist

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.
  • HY-P2518A
    Protease-Activated Receptor-1, PAR-1 Agonist TFA

    Protease-Activated Receptor (PAR) Cancer
    Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.
  • HY-P2519
    Protease-Activated Receptor-3 (PAR-3) (1-6), human

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide.
  • HY-P2519A
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide.
  • HY-P2344
    HIV Protease Substrate 1

    HIV Protease Infection
    HIV Protease Substrate 1, a fiuorogenic HIV protease substrate, can be used to study enzymatic activity of HIV protease.
  • HY-P2344A
    HIV Protease Substrate 1 TFA

    HIV Protease Infection
    HIV Protease Substrate 1 TFA, a fiuorogenic HIV protease substrate, can be used to study enzymatic activity of HIV protease.
  • HY-P2502
    Hepatitis Virus C NS3 Protease Inhibitor 2

    HCV Protease HCV Infection
    Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM.
  • HY-21141
    Cysteine protease inhibitor-2

    Cathepsin Cancer
    Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
  • HY-17541A
    Cysteine Protease inhibitor hydrochloride

    Cathepsin Others
    Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
  • HY-17541
    Cysteine Protease inhibitor

    Cathepsin Others
    Cysteine Protease inhibitor is an inhibitor of cysteine protease.
  • HY-126973
    BI-1230

    HCV Protease Infection
    BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity.
  • HY-108285
    (Rac)-Telmesteine

    Others Inflammation/Immunology
    (Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents.
  • HY-N7672
    Isoeuphorbetin

    HCV Protease Infection
    Isoeuphorbetin, a dimeric coumarin isolated from Viola philippica, is a potent HCV protease inhibitor with an IC50 of 3.63 µg/mL.
  • HY-N2355
    Solasurine

    Others Others
    Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 main protease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298.
  • 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-P0109A
    Z-FA-FMK

    (1S)-Z-FA-FMK

    SARS-CoV Infection
    Z-FA-FMK ((1S)-Z-FA-FMK; Compound 6) is a broad-spectrum halomethyl ketone inhibitor sgainst Coronavirus (SARS-CoV) main protease 3CL with a Ki of 25.7 μM.
  • HY-139080
    Atuzaginstat

    COR388

    Bacterial Neurological Disease
    Atuzaginstat (COR388) is an effective small-molecule bacterial protease lysine gingipain inhibitor and can be used for the research of Alzheimer's disease.
  • HY-139080A
    Atuzaginstat hydrochloride

    COR388 hydrochloride

    Bacterial Neurological Disease
    Atuzaginstat (COR388) hydrochloride is an effective small-molecule bacterial protease lysine gingipain inhibitor and can be used for Alzheimer's disease research.
  • HY-N9528
    Lyciumin A

    Angiotensin-converting Enzyme (ACE) Renin Cardiovascular Disease
    Lyciumin A, a cyclic octapeptide, exhibits inhibitory activity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension.
  • HY-N2565
    Rosamultin

    HIV Protease Infection
    Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. Rosamultin has inhibitory effects against HIV-1 protease. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects.
  • HY-P1436
    Acetyl-pepstatin

    HIV Infection
    Acetyl-pepstatin is a potent classical inhibitor of aspartic proteases (PRs) with XMRV PR and HIV-1 PR Ki values of 712 nM and 13 nM.
  • HY-126085
    (±)-Alliin

    (±)-L-Alliin

    SARS-CoV Infection
    (±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro).
  • HY-136703
    Lopinavir Metabolite M-1

    HIV Protease Infection
    Lopinavir Metabolite M-1, an active metabolite of Lopinavir, inhibits HIV protease with a Ki of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro.
  • HY-136298A
    X77

    SARS-CoV Infection
    X77 is a potent non-covalent inhibitor of the main protease of SARS-CoV-2 (SARS-CoV-2 M pro). X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM.
  • HY-N9366
    Tumulosic acid

    Others Inflammation/Immunology
    Tumulosic acid, a triterpenoid, inhibits KLK5 protease activity (IC50= 14.84 μM). Tumulosic acid suppresses the proteolytic processing of LL-37 in keratinocytes at ≤10 μM.
  • HY-100211
    TAPI-2

    TNF protease Inhibitor 2

    MMP SARS-CoV Cancer
    TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
  • HY-136298
    (Rac)-X77

    SARS-CoV Infection
    (Rac)-X77 is a racemate of X77. X77 is a potent non-covalent inhibitor of the main protease of SARS-CoV-2 (SARS-CoV-2 M pro). X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM.
  • HY-108137
    Z-LVG-CHN2

    Cathepsin HSV SARS-CoV Infection Inflammation/Immunology
    Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease.
  • HY-P0078
    TRAP-6

    PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
  • HY-B0182
    Carmofur

    HCFU

    Nucleoside Antimetabolite/Analog SARS-CoV Virus Protease Cancer
    Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC50 of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC50 of  24.3  μM.
  • HY-114080A
    Patamostat mesylate

    E-3123 mesylate

    Ser/Thr Protease Inflammation/Immunology
    Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis.
  • HY-114080
    Patamostat

    E-3123

    Ser/Thr Protease Inflammation/Immunology
    Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis.
  • HY-12946
    BI 653048

    Glucocorticoid Receptor Cytochrome P450 HCV Protease Infection Inflammation/Immunology
    BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
  • HY-12946A
    BI 653048 phosphate

    Glucocorticoid Receptor Cytochrome P450 HCV Protease Infection Inflammation/Immunology
    BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
  • HY-15287
    Nelfinavir

    AG1341

    HIV Protease HIV Infection Cancer
    Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.
  • HY-15287A
    Nelfinavir Mesylate

    AG 1343 Mesylate

    HIV Protease HIV Cancer Infection
    Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.
  • HY-N8471
    Niazinin

    Parasite SARS-CoV Infection Inflammation/Immunology
    Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity.
  • HY-W018781
    Benzamidine hydrochloride

    Ser/Thr Protease Cancer
    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
  • HY-119293
    K777

    Cathepsin CCR Cytochrome P450 Cancer Infection
    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-125959
    Ucf-101

    Apoptosis Neurological Disease Cardiovascular Disease
    Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.
  • HY-131905S
    BMS-986144

    HCV Protease HCV Cancer Infection Inflammation/Immunology
    BMS-986144 is a third-generation, pan-genotype (GT) NS3/4A protease inhibitor. BMS-986144 inhibits HCV replicon with EC50s of 2.3, 0.7, 1.0, 12, 8.0, and 5.8 nM for GT-1a, GT-1b, GT-2a, GT-3a, 1a R155X, and 1b D168V, respectively. BMS-986144 has the potential for the research of HCV infection.
  • HY-134595
    SENP1-IN-2

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-2 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 30. SENP1-IN-2 is developed for tumor radiosensitivity enhancement.
  • HY-134594
    SENP1-IN-1

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.
  • HY-134597
    SENP1-IN-4

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement.
  • HY-134596
    SENP1-IN-3

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement.
  • HY-108462
    ML-SA1

    TRP Channel Infection
    ML-SA1, as a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.
  • HY-P0018
    Pepstatin

    Pepstatin A

    Proteasome HIV Protease Autophagy Infection Cancer
    Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-P0018A
    Pepstatin Trifluoroacetate

    Pepstatin A Trifluoroacetate

    Proteasome HIV Protease Infection
    Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-P0018B
    Pepstatin Ammonium

    Pepstatin A Ammonium

    Proteasome HIV Protease Cancer Infection
    Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-101877
    Statine

    (3S,4S)-Statine; (S,S)-Statine

    Others Endocrinology
    Statine is an unusual amino acid that occurs twice in the sequence of pepstatin, a protease inhibitor that is active against pepsin and other acid proteases.
  • HY-17041
    Darunavir Ethanolate

    TMC114 Ethanolate

    HIV HIV Protease Infection
    Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
  • HY-19236
    PNU-103017

    HIV Protease HIV Infection
    PNU-103017 is an HIV protease inhibitor.
  • HY-113953
    Z-Asp-CH2-DCB

    Caspase Inflammation/Immunology
    Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
  • HY-10300
    Narlaprevir

    SCH 900518

    HCV HCV Protease SARS-CoV Infection
    Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.3 μM.
  • HY-17003
    Saquinavir Mesylate

    Ro 31-8959/003

    HIV HIV Protease Autophagy Infection Cancer
    Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy.
  • HY-B0385
    Gabexate mesylate

    FOY

    Factor Xa Proteasome Inflammation/Immunology
    Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .
  • HY-G0009
    Ritonavir metabolite

    Desthiazolylmethyloxycarbonyl Ritonavir

    Drug Metabolite Infection
    Ritonavir metabolite is a metabolite of Ritonavir, which is a HIV protease inhibitor.
  • HY-U00261
    L-689502

    HIV Protease Inflammation/Immunology
    L-689502 is a potent inhibitor of HIV-l protease with an IC50 of 1 nM.
  • HY-136573
    5-Hydroxytoluene-2,4-disulphonic acid diammonium

    Virus Protease Infection
    5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-136575
    4-Hydroxy-2-methylbenzenesulfonic acid ammonium

    Virus Protease Infection
    4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-136574
    2-Hydroxy-4-methylbenzenesulphonic acid ammonium

    Virus Protease Infection
    2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-100227
    E 64c

    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-12821
    AEBSF hydrochloride

    Thrombin Influenza Virus Others
    AEBSF hydrochloride is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin.
  • HY-N2006
    Ganoderic acid B

    HIV Protease Infection
    Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
  • HY-B0496
    PMSF

    Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride

    Cathepsin Others
    PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
  • HY-N2360
    Hinokiflavone

    E1/E2/E3 Enzyme Cancer
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
  • HY-112558
    AZ3451

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  • HY-P1260
    FSLLRY-NH2

    Protease-Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-U00282
    Chymase-IN-2

    Others Inflammation/Immunology
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
  • HY-P1006
    Ac-DEVD-pNA

    Others Others
    Ac-DEVD-pNA is a colorimetric substrate for caspase-3 (CPP32) and related cysteine proteases.
  • HY-122700
    Factor D inhibitor 6

    Complement System Inflammation/Immunology
    Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
  • HY-P1260A
    FSLLRY-NH2 TFA

    Protease-Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-P1645
    Papain

    Cathepsin Inflammation/Immunology
    Papain is a cysteine protease of the peptidase C1 family, which is used in food, pharmaceutical, textile, and cosmetic industries.
  • HY-17540
    HBX 19818

    Deubiquitinase Cancer
    HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.
  • HY-117793
    I-191

    Protease-Activated Receptor (PAR) Cancer
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-B0689
    Indinavir

    MK-639; L-735524

    HIV HIV Protease Inflammation/Immunology
    Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
  • HY-15148
    Tipranavir

    PNU-140690

    HIV Protease HIV SARS-CoV Infection
    Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL pro activity.
  • HY-14351
    AC-264613

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5.
  • HY-50736
    DUB-IN-1

    Deubiquitinase Cancer
    DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
  • HY-13447A
    PF429242 dihydrochloride

    Fatty Acid Synthase (FASN) Virus Protease Infection Metabolic Disease
    PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM.
  • HY-15282
    E-64

    Proteinase inhibitor E 64

    Cathepsin Autophagy Bacterial Inflammation/Immunology Cancer
    E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
  • HY-U00346
    DPP-IV-IN-1

    Dipeptidyl Peptidase Metabolic Disease
    DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
  • HY-19400
    DPC-681

    DPH-153893

    HIV Protease HIV Infection
    DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.
  • HY-B2196
    Gastric mucin

    Bacterial Antibiotic Infection Metabolic Disease
    Gastric mucin is a large glycoprotein which is thought to play a major role in the protection of the gastrointestinal tract from acid, proteases, pathogenic microorganisms, and mechanical trauma.
  • HY-112716
    N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride

    Others Cancer
    N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
  • HY-17367A
    Atazanavir sulfate

    BMS-232632 sulfate

    HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Cancer Infection
    Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM.
  • HY-17367
    Atazanavir

    BMS-232632

    HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Infection Cancer
    Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM.
  • HY-17431
    Fosamprenavir Calcium Salt

    GW433908G

    HIV Infection
    Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-78726
    Fosamprenavir

    Amprenavir phosphate; GW 433908

    HIV Infection
    Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-112128
    USP7-IN-3

    Deubiquitinase Cancer
    USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.
  • HY-10235
    Telaprevir

    VX-950

    HCV Protease HCV SARS-CoV Infection
    Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-14588
    Lopinavir

    ABT-378

    HIV HIV Protease SARS-CoV Infection
    Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity. Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM.
  • HY-P1449
    Boc-Gly-Gly-Phe-Gly-OH

    ADC Linker Cancer
    Boc-Gly-Gly-Phe-Gly-OH, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC).
  • HY-N0556
    Isoescin IA

    HIV Protease Infection
    Isoescin IA is a triterpenoid saponin isolated from the seeds of Aesculus chinensis. Isoescin IA has anti-HIV-1 protease activity.
  • HY-N8205
    Hispidulin 4'-O-β-D-glucopyranoside

    SARS-CoV Infection Inflammation/Immunology
    Hispidulin 4'-O-β-D-glucopyranosid, a natural compound, may serve as a potential COVID-19 main protease inhibitor.
  • HY-15667
    P005091

    P5091

    Deubiquitinase Cancer
    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
  • HY-116815
    Lalistat 1

    Bacterial Infection Neurological Disease
    Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease.
  • HY-19840
    Voxilaprevir

    GS-9857

    HCV Protease Infection
    Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-138558
    PAR-2-IN-1

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    PAR-2-IN-1 is a protease-activated receptor-2 (PAR2) signaling pathway inhibitor with anti-inflammatory and anticancer effects.
  • HY-P1449A
    Boc-Gly-Gly-Phe-Gly-OH TFA

    ADC Linker Cancer
    Boc-Gly-Gly-Phe-Gly-OH TFA, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC).
  • HY-33900
    Dihydrofuran-3(2H)-one

    3-Oxotetrahydrofuran

    Others Others
    Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is used for synthesizing cyclic ketone inhibitors that inhibits the serine protease plasmin.
  • HY-16709
    USP7-IN-1

    Deubiquitinase Cancer
    USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
  • HY-100229
    Aloxistatin

    E64d; E64c ethyl ester

    Cathepsin SARS-CoV Neurological Disease
    Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
  • HY-125169
    NSC 185058

    Cathepsin Autophagy Cancer
    NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity.
  • HY-17007
    Saquinavir

    Ro 31-8959

    HIV HIV Protease SARS-CoV Infection Cancer
    Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.36 μM.
  • HY-112818
    S130

    Cathepsin Autophagy Apoptosis Cancer
    S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux.
  • HY-90001
    Ritonavir

    ABT 538; RTV

    HIV Protease HIV SARS-CoV Apoptosis Infection
    Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM.
  • HY-18964
    MG-101

    Calpain inhibitor I; Ac-LLnL-CHO; ALLN

    Proteasome Cancer
    MG-101 is a potent 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.
  • HY-15148S
    Tipranavir-d4

    HIV Protease HIV SARS-CoV Infection
    Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL pro activity.
  • HY-15981
    Omarigliptin

    MK-3102

    Dipeptidyl Peptidase Metabolic Disease
    Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM).
  • HY-114164
    Thrombin (MW 37kDa)

    Thrombin Neurological Disease
    Thrombin (MW 37kDa) is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins.
  • HY-13865
    P 22077

    Deubiquitinase Cancer
    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.
  • HY-14588S1
    Lopinavir-d8

    HIV HIV Protease SARS-CoV Infection
    Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity. Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM.
  • HY-N3502
    20(21)-Dehydrolucidenic acid A

    HIV Protease Infection
    20(21)-Dehydrolucidenic acid A is a triterpenoid isolated from the fruiting body of the fungus Ganoderma sinense. 20(21)-Dehydrolucidenic acid A has weak anti-HIV-1 protease activity.
  • 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-139399
    JNJ-67856633

    MALT1 Cancer
    JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis.
  • HY-117043
    GRL0617

    Deubiquitinase SARS-CoV Infection
    GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro)/deubiquitinase, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM.
  • HY-114233
    MC-GGFG-DX8951

    Drug-Linker Conjugates for ADC Cancer
    MC-GGFG-DX8951 is a drug-linker conjugate for ADC with antitumor activity by using DX8951 (a DNA topoisomerase I inhibitor), linked via the protease cleavable MC-GGFG linker.
  • HY-17430
    Amprenavir

    VX-478

    HIV HIV Protease SARS-CoV Infection Cancer
    Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.09 μM.
  • HY-19303
    CRA-2059

    Ser/Thr Protease Inflammation/Immunology
    CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
  • HY-114996
    ADAMTS-5 Inhibitor

    Others Inflammation/Immunology
    ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
  • HY-19303A
    CRA-2059 hydrochloride

    Ser/Thr Protease Inflammation/Immunology
    CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
  • HY-129168
    USP7-IN-5

    Deubiquitinase Cancer
    USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
  • HY-128971
    LHVS

    Cathepsin Parasite Infection
    LHVS is a potent, non-selective cysteine protease inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
  • HY-129169
    USP7-IN-6

    Deubiquitinase Cancer
    USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
  • HY-B0190A
    Nafamostat mesylate

    FUT-175

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease Cancer
    Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..
  • HY-B0190
    Nafamostat

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2.
  • HY-100472
    ZYZ-488

    Caspase Cancer
    ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
  • HY-B0190B
    Nafamostat hydrochloride

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..
  • HY-N1910
    4'-O-Methylbavachalcone

    SARS-CoV Infection
    4'-O-Methylbavachalcone is a chalcone isolated from Psoralea corylifolia, inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) activity, with an IC50 of 10.1 μM.
  • HY-D0843
    N-Ethylmaleimide

    NEM

    Cathepsin Deubiquitinase Others
    N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
  • HY-18234A
    Leupeptin hemisulfate

    Cathepsin Inflammation/Immunology
    Leupeptin hemisulfate is a membrane-permeable thiol protease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion. Leupeptin hemisulfate also exhibits anti-inflammatory effect.
  • HY-P1313A
    PAR 4 (1-6) (TFA)

    GYPGQV TFA

    Protease-Activated Receptor (PAR) Others
    PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF-3; ZP10

    Virus Protease HSV HIV Cancer Infection
    Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 µM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent.
  • HY-127039
    Antipain

    Ser/Thr Protease DNA/RNA Synthesis Cancer Metabolic Disease
    Antipain is a protease inhibitor isolated from Actinomycetes. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain restricts uterine DNA synthesis and function in mice.
  • HY-127034
    Antipain dihydrochloride

    Ser/Thr Protease DNA/RNA Synthesis Cancer Metabolic Disease
    Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice.
  • HY-17542
    PLpro inhibitor

    SARS-CoV Infection
    PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
  • HY-111532
    (3R,4R)-A2-32-01

    Bacterial Infection
    (3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
  • HY-13487
    USP7/USP47 inhibitor

    Deubiquitinase Cancer
    USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
  • HY-18200
    Atopaxar

    E5555; ER-172594-00

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
  • HY-17634
    Glecaprevir

    ABT-493

    HCV HCV Protease SARS-CoV Infection
    Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 4.09 μM.
  • HY-112254
    ZINC03129319

    Virus Protease Infection
    ZINC03129319 is a dengue virus (DENV) NS2B-NS3 protease inhibitor extracted from patent US20150141521A1, has inhibition constants (Ki1) of 92 μM and Ki3 of 20 μM.
  • HY-126361
    ZK824190

    Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  • HY-B0689A
    Indinavir sulfate

    MK-639 sulfate; L735524 sulfate

    HIV HIV Protease SARS-CoV Infection
    Indinavir sulfate(MK-639 sulfate; L735524 sulfate ) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability. Indinavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.71 μM.
  • HY-13512
    Camostat mesylate

    Camostat mesilate; FOY305; FOY-S980

    Ser/Thr Protease SARS-CoV Infection Inflammation/Immunology
    Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
  • HY-121282A
    Mepazine hydrochloride

    Pecazine hydrochloride

    MALT1 Apoptosis Cancer
    Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis.
  • HY-138687
    PF-07321332

    SARS-CoV Infection Inflammation/Immunology
    PF-07321332 is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor . PF-07321332 targets to the SARS-CoV-2 virus and can be used for COVID-19 reseacrch.
  • HY-18236
    MDL-28170

    Calpain Inhibitor III

    Proteasome Inflammation/Immunology Neurological Disease
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.
  • HY-121282
    Mepazine

    Pecazine

    MALT1 Apoptosis Cancer
    Mepazine (Pecazine) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
  • HY-N6773
    Cytochalasin A

    HIV Protease Fungal Infection
    Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.
  • HY-19837
    BMS-986120

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
  • HY-111350
    FT827

    Deubiquitinase Cancer
    FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.
  • HY-120528A
    GB-110 hydrochloride

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-14434
    Asunaprevir

    BMS-650032

    HCV HCV Protease SARS-CoV Infection
    Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM. Asunaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-10241
    Simeprevir

    TMC435

    HCV HCV Protease SARS-CoV Infection
    Simeprevir (TMC435) is an oral and potent HCV NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-120528
    GB-110

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-B0372A
    Bromhexine hydrochloride

    SARS-CoV Autophagy HIV Metabolic Disease
    Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.
  • HY-10238
    Danoprevir

    ITMN-191; R7227; RO5190591; RG7227

    HCV Protease HCV SARS-CoV Infection
    Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM). Danoprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 0.05 μM.
  • HY-17007S
    Saquinavir-d9

    HIV HIV Protease SARS-CoV Infection Cancer
    Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir. Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.36 μM.
  • HY-10119
    Vorapaxar

    SCH 530348

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-90001S
    Ritonavir-d6

    HIV Protease HIV SARS-CoV Apoptosis Infection
    Ritonavir-d6 (ABT 538-d6) is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM.
  • HY-138540
    1-Dodecylimidazole

    N-Dodecylimidazole

    Fungal Cancer
    1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity.
  • HY-13965
    Parmodulin 2

    ML161

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-109571
    HZ-1157

    HCV Protease Infection Inflammation/Immunology
    HZ-1157 inhibits HCV NS3/4A protease with an IC50 of 1.0 μmol/L. HZ-1157 (4a) has a high dengue virus inhibitory activity (EC50 = 0.15 μM) and is a relatively nontoxic (CC50 > 10 μM) dengue antiviral agent.
  • HY-15287S
    Nelfinavir-d3

    HIV Protease HIV Infection Cancer
    Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.
  • HY-11091
    Razaxaban hydrochloride

    BMS 561389 hydrochloride; DPC 906 hydrochloride

    Factor Xa Thrombin Cardiovascular Disease
    Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
  • HY-10119A
    Vorapaxar sulfate

    SCH 530348 sulfate

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-124748A
    ENMD-1068 hydrochloride

    Protease-Activated Receptor (PAR) Inflammation/Immunology Cardiovascular Disease
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction.
  • HY-N0554
    Escin IA

    HIV Protease Cancer Infection
    Escin IA is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression.
  • HY-12594
    Paritaprevir

    ABT-450; Veruprevir

    HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM.
  • HY-10237
    Boceprevir

    EBP 520; SCH 503034

    HCV Protease HCV SARS-CoV Infection
    Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay. Boceprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-13765
    6-Thioguanine

    Thioguanine; 2-Amino-6-purinethiol

    SARS-CoV Deubiquitinase DNA Methyltransferase Autophagy Apoptosis Endogenous Metabolite Cancer Infection Inflammation/Immunology
    6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
  • HY-100415
    UKI-1

    UKI-1C

    PAI-1 Ser/Thr Protease Cancer
    UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
  • HY-123517
    DC07090 dihydrochloride

    Enterovirus Infection
    DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM.
  • HY-19269
    FK706

    Elastase Inflammation/Immunology
    FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.
  • HY-117370
    USP25/28 inhibitor AZ1

    AZ1

    Deubiquitinase Cancer
    USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
  • HY-17040
    Darunavir

    TMC114; UIC-94017

    HIV HIV Protease Infection Inflammation/Immunology
    Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity.
  • HY-134817
    USP7-IN-8

    Deubiquitinase Cancer
    USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.
  • HY-106161
    Rupintrivir

    AG7088

    Virus Protease Enterovirus Infection Inflammation/Immunology
    Rupintrivirvr (AG7088), an antiviral drug, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect.
  • HY-107662
    TCS PrP Inhibitor 13

    Apoptosis Cancer Infection
    TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrP C) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis.
  • HY-128345
    UDM-001651

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP).
  • HY-W088075
    Acriflavine hydrochloride

    Acriflavinium chloride hydrochloride

    HIF/HIF Prolyl-Hydroxylase Bacterial SARS-CoV Cancer Infection
    Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic. Acriflavine hydrochloride is a potent HIF-1 inhibitor, with antitumor activity. Acriflavine hydrochloride has antimicrobial and antiviral activities. Acriflavine hydrochloride is a potent papain-like protease (PL pro) inhibitor, which inhibits SARS-CoV-2
  • 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 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.
  • HY-107123
    TMC310911

    HIV Protease Infection
    TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.
  • HY-137048
    PF-00835231

    SARS-CoV Infection
    PF-00835231 is a CoV-2 cysteine 3C-like protease (3CL pro) inhibitor, with IC50s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CL pro, respectively. PF-00835231 is developed for the research of anti-SARS-CoV-2/COVID-19.
  • HY-111532B
    (3S,4S)-A2-32-01

    Others Infection
    (3S,4S)-A2-32-01 is a less active S-enantiomer of (3R,4R)-A2-32-01. (3R,4R)-A2-32-01 is an anti-virulence agent and a specific caseinolytic protein proteases (ClpP) inhibitor.
  • HY-N7073
    Silymarin

    SARS-CoV Cancer Infection Inflammation/Immunology Neurological Disease
    Silymarin is an extract of the milk thistle (Silybum marianum). Silymarin can significantly reduce tumor cell proliferation, angiogenesis as well as insulin resistance. Silymarin, a food-derived antiviral molecule, is an effective SARS-CoV-2 main protease (M pro) inhibitor. Silymarin has the chemopreventive effect on hepatocellular carcinoma (HCC). Silymarin has the potential for COVID-19 research.
  • HY-10472
    LY2811376

    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-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 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.
  • HY-N6856
    4-Hydroxycoumarin

    Endogenous Metabolite Bacterial Infection
    4-Hydroxycoumarin, a coumarin derivative, is one of the most versatile heterocyclic scaffolds and is frequently applied in the synthesis of various organic compounds. 4-Hydroxycoumarin possesses both electrophilic and nucleophilic properties. 4-Hydroxycoumarin derivatives are employed as the anticoagulant, antibacterial, antifungal, antiviral, antitumor, antiprotozoal, insecticidal, antimycobacterial, antimutagenic, antioxidant, anti-inflammatory agents, HIV protease inhibitors and tyrosine kinase inhibitors.
  • HY-N2996
    Ganodermanondiol

    HIV Protease Infection
    Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum.Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity. Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC50 of 90 μM. Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC50 of 41.7μM.
  • HY-14350
    AC-55541

    Protease-Activated Receptor (PAR) Others
    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca 2+ mobilization assays and exhibits pronociceptive activity in vivo.
  • HY-128570
    FD-IN-1

    Complement System Inflammation/Immunology
    FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively.
  • HY-138078
    Lufotrelvir

    PF-07304814

    SARS-CoV Infection
    Lufotrelvir (PF-07304814), a phosphate prodrug of PF-00835231, acts as a potent 3CL pro protease (M pro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CL pro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle.
  • HY-12276
    MALT1 inhibitor MI-2

    MALT1 Cancer
    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
  • HY-134820
    MLT-943

    MALT1 Inflammation/Immunology
    MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.
  • HY-15298C
    Grazoprevir sodium salt

    MK-5172 sodium salt

    HCV HCV Protease SARS-CoV Infection
    Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir sodium salt inhibits SARS-CoV-2 3CL pro activity.
  • HY-15298B
    Grazoprevir hydrate

    MK-5172 hydrate

    HCV HCV Protease SARS-CoV Infection
    Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir hydrate inhibits SARS-CoV-2 3CL pro activity.
  • HY-107146
    PZ-128

    P1pal-7

    Protease-Activated Receptor (PAR) Cancer Cardiovascular Disease
    PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.
  • HY-15298
    Grazoprevir

    MK-5172

    HCV Protease HCV SARS-CoV Infection
    Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-15298A
    Grazoprevir potassium salt

    MK-5172 potassium salt

    HCV HCV Protease SARS-CoV Infection
    Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir potassium salt inhibits SARS-CoV-2 3CL pro activity.
  • HY-15589
    GW9508

    GPR40 Potassium Channel Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
  • HY-14994
    SCH79797 dihydrochloride

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-124322
    NB-360

    Beta-secretase Inflammation/Immunology Neurological Disease
    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-19369
    L-685458

    L-685,458

    γ-secretase Apoptosis Neurological Disease Cancer
    L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers.