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Pathways Recommended: Metabolic Enzyme/Protease
Results for "

Proteases Inhibitors

" in MCE Product Catalog:

316

Inhibitors & Agonists

1

Screening Libraries

1

Fluorescent Dye

1

Biochemical Assay Reagents

17

Peptides

4

MCE Kits

2

Inhibitory Antibodies

31

Natural
Products

19

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-150691
    SARS 3CLpro-IN-1

    SARS-CoV Cancer
    SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomer of the octahydroisochromene scaffold, directs the P1 site imidazole.
  • HY-145435
    SARS-CoV-2-IN-12

    SARS-CoV Infection
    SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19.
  • HY-144820
    JO146

    Ser/Thr Protease Infection
    JO146 is a Chlamydia trachomatis high temperature requirement A (CtHtrA) protease inhibitor with IC50s of 21.86 and 1.15 μM for CtHtrA and human neutrophil elastase (HNE), respectively. JO146 can be used to inhibits bacterial infections.
  • HY-15899
    Des(benzylpyridyl) Atazanavir

    HIV Protease HIV Drug Metabolite Infection
    Des(benzylpyridyl) Atazanavir (compound M1) is a N-dealkylation product of Atazanavir (HY-17367) metabolite. Atazanavir is a highly selective HIV-1 protease inhibitor. Des(benzylpyridyl) Atazanavir may contribute to the effectiveness Atazanavir but also to the toxicity and interactions. Des(benzylpyridyl) Atazanavir can be used for further research of Atazanavir effects.
  • HY-124379
    TPCK

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    Ser/Thr Protease HPV Cancer Inflammation/Immunology
    TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium.
  • 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-P0018C
    Pepstatin acetate

    Pepstatin A acetate

    HIV Protease Autophagy Infection Inflammation/Immunology
    Pepstatin (Pepstatin A) acetate is a specific, orally active 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 acetate also inhibits HIV protease.
  • HY-P0018
    Pepstatin

    Pepstatin A

    HIV Protease Autophagy Infection Inflammation/Immunology
    Pepstatin (Pepstatin A) is a specific, orally active 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 also inhibits HIV protease.
  • HY-P0018A
    Pepstatin Trifluoroacetate

    Pepstatin A Trifluoroacetate

    HIV Protease Autophagy Infection Inflammation/Immunology
    Pepstatin (Pepstatin A) Trifluoroacetate is a specific, orally active 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 Trifluoroacetate also inhibits HIV protease.
  • HY-P0018B
    Pepstatin Ammonium

    Pepstatin A Ammonium

    HIV Protease Autophagy Infection Inflammation/Immunology
    Pepstatin (Pepstatin A) Ammonium is a specific, orally active 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-18234
    Leupeptin

    Ser/Thr Protease Virus Protease Cathepsin Infection Inflammation/Immunology
    Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits M pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.
  • HY-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-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-18234A
    Leupeptin hemisulfate

    Cathepsin Ser/Thr Protease Virus Protease Infection Inflammation/Immunology
    Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits M pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.
  • HY-B0385
    Gabexate mesylate

    FOY

    Factor Xa Proteasome Inflammation/Immunology
    Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .
  • 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-W129596
    Policresulen

    Virus Protease Infection
    Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease (IC50 of 0.48 μg/mL). Policresulen inhibits DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL. Policresulen acts as a competitive inhibitor of the protease, and slightly affects the protease stability.
  • HY-19236
    PNU-103017

    HIV Protease HIV Infection
    PNU-103017 is an HIV protease inhibitor.
  • HY-144646
    SP-471

    Virus Protease Infection
    SP-471 is a potent dengue virus (DENV) protease inhibitor with IC50 value of 18 μM. SP-471 inhibits both intermolecular and intramolecular protease processes of DENV.
  • HY-151197
    HIV protease-IN-1

    HIV Protease Infection
    HIV protease-IN-1 (compound 1·succinate) is a potent HIV protease non-peptidic inhibitor, can be used to research AIDS.
  • 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-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-146888
    HIV-1 protease-IN-2

    HIV Protease Infection
    HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants.
  • 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-G0009
    Ritonavir metabolite

    Desthiazolylmethyloxycarbonyl Ritonavir

    Drug Metabolite Infection
    Ritonavir metabolite is a metabolite of Ritonavir, which is a HIV protease inhibitor.
  • HY-121240
    Brecanavir

    GW640385

    HIV Protease Infection
    Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.
  • HY-147650
    HIV-1 protease-IN-5

    HIV Protease Infection
    HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants.
  • 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-100397
    Elastatinal

    Elastase Inflammation/Immunology
    Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease.
  • 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-144644
    NS2B/NS3-IN-3

    Virus Protease Infection
    NS2B/NS3-IN-3 (Compd 66) is an inhibitor of Flavivirus NS2B-NS3 protease.
  • 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-146012
    HIV-1 protease-IN-4

    HIV Infection
    HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a prodrug of atazanavir. HIV-1 protease-IN-4 as a prodrug that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent drug.
  • HY-144688
    HIV-1 protease-IN-1

    HIV Infection
    HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie[1].
  • HY-12821
    AEBSF hydrochloride

    Thrombin Influenza Virus Ser/Thr Protease Others
    AEBSF hydrochloride is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin.
  • HY-151250
    HIV-1 protease-IN-7

    HIV Protease Infection
    HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor (IC50=3.52 nM, EC50=37 nM).
  • HY-P1260
    FSLLRY-NH2

    Protease Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-N2360
    Hinokiflavone

    E1/E2/E3 Enzyme Apoptosis 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-150549
    HIV-1 protease-IN-6

    HIV Protease HIV Infection Inflammation/Immunology
    HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus.
  • HY-144813
    Gü2602

    Cathepsin Cancer Inflammation/Immunology
    Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
  • HY-144812
    Gü1303

    Cathepsin Cancer Inflammation/Immunology
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
  • 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-P1260A
    FSLLRY-NH2 TFA

    Protease Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • 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-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-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-19232
    R-87366

    HIV Protease Inflammation/Immunology
    R-87366 is a water-soluble human immunodeficiency virus (HIV) protease inhibitor. R-87366 has potent inhibitory for HIV protease with a Ki value of 11 nM. R-87366 can be used for the research of anti-human immunodeficiency virus (HIV).
  • 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-120880
    SKF107457

    HIV Protease Infection
    SKF107457 is an HIV-1 protease inhibitor that can be used in AIDS research.
  • HY-145349
    FXIa-IN-6

    Factor Xa Cardiovascular Disease
    FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases (Ki = 0.3 nM).
  • 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-10242
    Ciluprevir

    BILN 2061; BILN 2061ZW

    HCV HCV Protease Infection
    Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.
  • HY-17367A
    Atazanavir sulfate

    BMS-232632 sulfate

    HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite 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 Endogenous Metabolite 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-152200
    HIV-1 inhibitor-53

    HIV Protease Reverse Transcriptase Infection Inflammation/Immunology
    HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS).
  • 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-137565
    Hydroxy ritonavir

    Drug Metabolite Others
    Hydroxy ritonavir is a metabolite of Ritonavir. Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS.
  • HY-147020
    Coronastat

    NK01-63

    SARS-CoV Infection
    Coronastat is a potent inhibitor of the SARS-CoV-2 3CL protease. The SARS-CoV-2 3CL protease is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle.
  • 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-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-17367S4
    Atazanavir-d6

    BMS-232632-d6

    HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d6 is deuterium labeled Atazanavir. 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 3CLpro inhibitor with an IC50 of 3.49 μM.
  • HY-17367S3
    Atazanavir-d5

    HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d5 is the deuterium labeled Atazanavir. 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-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-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-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-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-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-144742
    NS2B/NS3-IN-6

    Virus Protease Infection
    NS2B/NS3-IN-6 (Compound 1a) is an allosteric DENV and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 2.23 µM and 25.2 µM against ZIKV and DENV proteases, respectively.
  • HY-150784
    XR8-89

    SARS-CoV Infection
    XR8-89 is a potent papain-like protease (PL pro) inhibitor with an IC50 value of 0.1 μM. XR8-89 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. XR8-89 can be used for SARS-CoV-2 research.
  • HY-150786
    PLP_Snyder530

    SARS-CoV Infection
    PLP_Snyder530 is a potent papain-like protease (PL pro) inhibitor with an IC50 value of 6.4 μM. PLP_Snyder530 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. PLP_Snyder530 can be used for SARS-CoV-2 research.
  • 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-I0179
    ITMN 4077

    HCV Protease Infection
    ITMN 4077 is a macrocyclic inhibitor against Hepatitis C Virus (HCV) NS3 protease (EC50: 2131 nM).
  • HY-10243
    Vaniprevir

    MK-7009

    HCV HCV Protease Infection
    Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
  • 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-146649
    LmCPB-IN-1

    Parasite Cathepsin Infection
    LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7.
  • HY-139732
    SARS-CoV-2-IN-8

    SARS-CoV Infection
    SARS-CoV-2-IN-8 is a SARS-CoV-2 main protease inhibitor with an IC50 value of 0.75 μM.
  • 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-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-100212
    JE-2147

    AG1776; KNI-764

    HIV HIV Protease Infection
    JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro.
  • 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-17431
    Fosamprenavir Calcium Salt

    GW433908G

    HIV Endogenous Metabolite 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 Endogenous Metabolite Infection
    Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-139866
    SARS-CoV-2-IN-9

    SARS-CoV Infection
    SARS-CoV-2-IN-9 is an inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease.
  • HY-115753
    Calpain Inhibitor-1

    Proteasome Neurological Disease
    Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC50=100 nM; Ki=2.89 μM).
  • 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-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-150783
    SARS-CoV-2-IN-24

    SARS-CoV Infection
    SARS-CoV-2-IN-24 (compound 7) is a potent papain-like protease (PL pro) inhibitor. SARS-CoV-2-IN-24 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. SARS-CoV-2-IN-24 can be used for SARS-CoV-2 research.
  • 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-17367S2
    Atazanavir-d9

    BMS-232632-d9

    HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d9 (BMS-232632-d9) is the deuterium labeled Atazanavir. 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-16593
    GS-9256

    HCV Protease Infection
    GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity.
  • HY-147845
    F8-S40

    SARS-CoV Infection
    F8-S40 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 10.88 μM.
  • 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-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-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-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-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-148481
    USP7-IN-10

    Deubiquitinase Cancer
    USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM.
  • HY-N4334
    Molassamide B

    Ser/Thr Protease Metabolic Disease
    Molassamide B is a serine protease inhibitor with IC50 values of 24.65, 11.69 and 5.42 nM against chymotrypsin, elastase and proteinase K, respectively.
  • HY-148310
    Flaviviruses-IN-2

    Virus Protease Infection
    Flaviviruses-IN-2 (compound 78) is a potent flaviviruses inhibitor. Flaviviruses-IN-2 reduces the WNV (West Nile virus) protease activity, with inhibition of 56%.
  • 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-10241
    Simeprevir

    TMC435; TMC435350

    HCV HCV Protease SARS-CoV DNA/RNA Synthesis Infection
    Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
  • 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-10241A
    Simeprevir sodium

    TMC435 sodium; TMC435350 sodium

    HCV HCV Protease SARS-CoV DNA/RNA Synthesis Infection
    Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
  • HY-N10582
    Aeruginosin 98-B

    Protease Activated Receptor (PAR) Thrombin Cancer Infection Metabolic Disease Inflammation/Immunology
    Aeruginosin 98-B is a protease inhibitor. Aeruginosin 98-B inhibits trypsin, plasmin and thrombin with IC50 values of 0.6, 7.0 and 10.0 μg/mL, respectively.
  • HY-N4330
    Rivulariapeptolides 1155

    Ser/Thr Protease Metabolic Disease
    Rivulariapeptolides 1155 is a potent serine protease inhibitor with IC50s of 41.84, 4.94, 56.54 nM for chymotrypsin, elastase, prpteinase K, respectively.
  • HY-151611
    UAMC-00050

    Ser/Thr Protease Inflammation/Immunology
    UAMC-00050 is a potent trypsin-like serine protease inhibitor. UAMC-00050 can be used in research of dry eye syndrome and ocular inflammation.
  • 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

    Autophagy Atg4 Cancer
    NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity.
  • HY-145263
    VD2173

    Ser/Thr Protease Cancer
    VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer.
  • 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-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-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-144740
    NS2B/NS3-IN-5

    Virus Protease Infection
    NS2B/NS3-IN-5 (Compound 25b) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.67 µM and 4.38 µM against ZIKV and DENV2 NS2B/NS3 proteases, respectively.
  • HY-144736
    NS2B/NS3-IN-4

    Virus Protease Infection
    NS2B/NS3-IN-4 (Compound 34e) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.69 µM and 1.04 µM against DENV2 and ZIKV NS2B/NS3 proteases, respectively.
  • HY-N4332
    Rivulariapeptolides 1121

    Ser/Thr Protease Cancer Infection
    Rivulariapeptolides 1121 is a high potent and selective serine protease inhibitor with IC50 values of 35.52 nM, 13.24 nM and 48.05 nM for chymotrypsin, elastase and proteinase K, respectively.
  • HY-N4331
    Rivulariapeptolides 1185

    Ser/Thr Protease Cancer Infection
    Rivulariapeptolides 1185 is a high potent and selective serine protease inhibitor with IC50 values of 13.17 nM, 23.59 nM and 55.26 nM for chymotrypsin, elastase and proteinase K, respectively.
  • HY-143423
    MALT1-IN-5

    MALT1 Cancer
    MALT1-IN-5 (compound 1) is a potent MALT1 protease inhibitor. MALT1-IN-5 can be used for cancer research.
  • 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-B0689S
    Indinavir-d6

    MK-639-d6 free base; L-735524-d6 free base

    HIV HIV Protease Inflammation/Immunology
    Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
  • 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-N4333
    Rivulariapeptolides 988

    Ser/Thr Protease Cancer Infection
    Rivulariapeptolides 988 is a high potent and selective serine protease inhibitor with IC50 values of 95.46 nM, 15.29 nM and 85.50 nM for chymotrypsin, elastase and proteinase K, respectively.
  • HY-128971
    LHVS

    Cathepsin Parasite Infection Neurological Disease
    LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM.
  • HY-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-147844
    F8-S43-S3

    SARS-CoV Infection
    F8-S43-S3 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 9.69 μM.
  • HY-143425
    MALT1-IN-7

    MALT1 Cancer
    MALT1-IN-7 (compound 142b) is a potent MALT1 protease inhibitor. MALT1-IN-7 has the potential for cancer research.
  • HY-143470
    SARS-CoV-2-IN-18

    SARS-CoV Infection
    SARS-CoV-2-IN-18 (Compound 26) is a potent SARS-CoV-2 3C-like protease inhibitor with an IC50 of 45 nM.
  • HY-152222
    SPR38

    SARS-CoV Cathepsin Infection
    SPR38 is a potent SARS-CoV-2 main protease inhibitor, with a Ki of 0.260 μM. SPR38 also inhibits hCatL and hCatB, with Ki values of 1.92 μM and 11.1 μM, respectively.
  • 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-143425A
    (R)-MALT1-IN-7

    MALT1 Cancer
    (R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor. (R)-MALT1-IN-7 has the potential for cancer research.
  • HY-148099
    USP1-IN-2

    Deubiquitinase Cancer
    USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM.
  • HY-143424
    MALT1-IN-6

    MALT1 Cancer
    MALT1-IN-6 is a potent MALT1 protease inhibitor with a Ki of 9 nM. MALT1-IN-6 has anticancer effects (WO2018226150A1; Compound 4).
  • HY-139399
    Safimaltib

    JNJ-67856633

    MALT1 Cancer
    Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis.
  • 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-10235S
    Telaprevir-d4

    VX-950-d4

    HCV Protease HCV SARS-CoV Infection
    Telaprevir-d4 (VX-950-d4) is the deuterium labeled Telaprevir. 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-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-78726S
    Fosamprenavir-d4

    Amprenavir phosphate-d4; GW 433908-d4

    HIV Endogenous Metabolite Infection
    Fosamprenavir-d4 is deuterium labeled Fosamprenavir. Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-150789
    SARS-CoV-2-IN-23

    SARS-CoV Infection
    SARS-CoV-2-IN-23 (compound GRL-0617) is a SARS-COV-2 papain-like protease (PLpro) inhibitor with an IC50 value of 2.3 μM.
  • 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-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-152009
    SARS-CoV-2 3CLpro-IN-7

    SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 1.4 µM.
  • 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-N2306
    Aclacinomycin A

    Aclarubicin

    Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic Cancer
    Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
  • HY-147031
    JAMM protein inhibitor 2

    Others Cancer
    JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2, respectively. JAMM protein inhibitor 2 can be used for researching anticancer
  • 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-111532
    (3R,4R)-A2-32-01

    Bacterial Infection
    (3R,4R)-A2-32-01 (compound 24(R,R)), the (R,R)-enantiomer of A2-32-01, is a Staphylococcus aureus caseinolytic protease (SaClpP) inhibitor.
  • 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-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-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-143216A
    Ensitrelvir fumarate

    S-217622 fumarate

    SARS-CoV Virus Protease Infection
    Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).
  • HY-143216
    Ensitrelvir

    S-217622

    SARS-CoV Virus Protease Infection
    Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).
  • 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-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-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-17430S1
    Amprenavir-d4-1

    VX-478-d4-1

    HIV HIV Protease SARS-CoV Infection Cancer
    Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 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-148072
    MM3122

    SARS-CoV Infection
    MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells.
  • HY-145277
    SARS-CoV-2-IN-11

    SARS-CoV Infection
    SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals.
  • HY-145276
    SARS-CoV-2-IN-10

    SARS-CoV Infection
    SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals.
  • HY-144464
    SARS-CoV-2 Mpro-IN-1

    SARS-CoV Infection
    SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective and irreversible inhibitor of SARS-CoV-2 main protease (Mpro), with an IC50 of 116 nM.
  • HY-18964
    MG-101

    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 Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
  • HY-D0843S
    N-Ethylmaleimide-d5

    NEM-d5

    Cathepsin Deubiquitinase Others
    N-Ethylmaleimide-d5 (NEM-d5) is the deuterium labeled N-Ethylmaleimide. 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-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-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-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-10241S
    Simeprevir-13C,d3

    TMC435-13C,d3; TMC435350-13C,d3

    HCV HCV Protease SARS-CoV DNA/RNA Synthesis Infection
    Simeprevir-13C,d3 (TMC435-13C,d3) is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
  • 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-152101
    LY1

    SARS-CoV Infection
    LY1 is a potent, selective and covalent inhibitor against both SARS-CoV-2 PL pro and M pro with Kd values of 1.5 μM and 2.3 μM for M pro C145A protein and PL pro C111A protein, respectively. LY1 potent against the viral proteases, with IC50s of 0.12 μM and 0.99 μM against M pro and PL pro. LY1 shows high selectivity over other kinases, human proteases and metalloenzyme.
  • 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-148482
    USP7-IN-11

    Deubiquitinase Cancer
    USP7-IN-11 is a potent ubiquitin-specific protease 7 (USP7) (Deubiquitinase) inhibitor with an IC50 of 0.37 nM. USP7-IN-11 has anticancer effects (WO2022048498A1; Example 187).
  • HY-151991
    SARS-CoV-2/MERS Mpro-IN-2

    SARS-CoV Infection
    SARS-CoV-2/MERS Mpro-IN-2 (compound 9d) is a potent SARS-CoV-2 and MERS main protease inhibitor with IC50 values of 0.21, 0.07 µM, respectively.
  • HY-151990
    SARS-CoV-2/MERS Mpro-IN-1

    SARS-CoV Infection
    SARS-CoV-2/MERS Mpro-IN-1 (compound 9c) is a potent SARS-CoV-2 and MERS main protease inhibitor with IC50 values of 0.10, 0.06 µM, respectively.
  • 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-17430S
    Amprenavir-d4

    HIV HIV Protease SARS-CoV Infection Cancer
    Amprenavir-d4 is the deuterium labeled Amprenavir. 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-B0689A
    Indinavir sulfate

    MK-639; L735524

    HIV HIV Protease SARS-CoV Apoptosis MMP Infection Cancer
    Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CL pro inhibitor.
  • HY-B0689
    Indinavir

    MK-639 free base; L-735524 free base

    HIV HIV Protease Apoptosis MMP SARS-CoV Inflammation/Immunology Cancer
    Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL pro inhibitor.
  • 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-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-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-111532B
    (3S,4S)-A2-32-01

    Others Infection
    (3S,4S)-A2-32-01 (compound 24(S,S)), a less active (S,S)-enantiomer of A2-32-01. A2-32-01 is a potent caseinolytic protein proteases (ClpP) inhibitor.
  • 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-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-143427
    MALT1-IN-9

    MALT1 Cancer
    MALT1-IN-9 is a potent MALT1 protease inhibitor with a IC50 of <500 nM in Raji MALT1-GloSensor cells. MALT1-IN-9 has anticancer effects (WO2021000855A1; Compound 5).
  • 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-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-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-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-D0843
    N-Ethylmaleimide

    NEM

    Cathepsin Deubiquitinase Apoptosis Others
    N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides.
  • 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-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-152224
    SPR41

    SARS-CoV Infection
    SPR41 is a potent SARS-CoV-2 main protease inhibitor with Ki values of 0.184, 0.252, 14.4 µM for SARS-CoV-2 M pro, hCatL, hCatB, respectively. SPR41 shows antiviral and cytotoxicity.
  • HY-152220
    SPR39

    SARS-CoV Infection
    SPR39 is a potent SARS-CoV-2 main protease inhibitor with Ki values of 0.252, 3.38, 7.88 µM for SARS-CoV-2 M pro, hCatL, hCatB, respectively. SPR39 shows antiviral and cytotoxicity.
  • HY-B0689B
    Indinavir sulfate ethanolate

    MK-639 ethanolate; L735524 ethanolate

    Apoptosis MMP HIV HIV Protease SARS-CoV Cancer Infection
    Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CL pro inhibitor.
  • 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-14853
    Darexaban

    YM150

    Factor Xa Ser/Thr Protease Cardiovascular Disease
    Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.
  • HY-146998
    SARS-CoV-2 3CLpro-IN-2

    SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-2 3CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases.
  • 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-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-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-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-143426
    MALT1-IN-8

    MALT1 Cancer
    MALT1-IN-8 is a potent MALT1 protease inhibitor with a IC50 of 2 nM. MALT1-IN-8 inhibits the growth of OCI-LY3 lymphoma cells with an IC50 of 1.16 μM. MALT1-IN-8 has anticancer effects (WO2018165385A1; Compound 8).
  • 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-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-103435
    Vialinin A

    Terrestrin A

    Deubiquitinase Cancer Inflammation/Immunology
    Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research.
  • HY-P99050
    Sutimlimab

    Complement System Inflammation/Immunology Cardiovascular Disease
    Sutimlimab, a first-in-class complement protein component 1, s subcomponent (C1s) inhibitor, can be used for the research of cold agglutinin disease. C1s is a serine protease which cleaves C4 and C2 to form the C3 convertase.
  • 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-138687
    Nirmatrelvir

    PF-07321332

    SARS-CoV Infection Inflammation/Immunology
    Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research.
  • HY-N1739
    Tectoquinone

    2-Methylanthraquinone

    SARS-CoV Virus Protease Infection
    Tectoquinone (2-Methylanthraquinone) is a SARSCoV-2 main protease inhibitor against COVID-19. Tectoquinone exhibits strong mosquito larvicidal activity with the LC50 values of 3.3 and 5.4 μg/ml against A. aegypti and A. albopictus in 24 h, respectively.
  • 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-117043
    GRL0617

    Deubiquitinase SARS-CoV Infection
    GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome.
  • HY-90001S1
    Ritonavir-13C,d3

    ABT 538-13C,d3; RTV-13C,d3

    HIV Protease HIV SARS-CoV Apoptosis Infection
    Ritonavir-13C,d3 (ABT 538-13C,d3) is the 13C- and 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-151376
    SAP2-IN-1

    Proteasome Infection
    SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection.
  • 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-101666
    HBX 41108

    Deubiquitinase Apoptosis Cancer
    HBX 41108 is an uncompetitive inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. HBX 41108 induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines.
  • 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-144648
    Mpro/PLpro-IN-1

    Others Infection
    Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of M pro/PL pro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus M pro (IC50 = 1.72 μM) and submicromolar potency versus PL pro (IC50 = 0.67 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-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-143422A
    (R)-MALT1-IN-3

    MALT1 Cancer
    (R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively.
  • 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-147516
    SARS-CoV-2-IN-21

    SARS-CoV Infection
    SARS-CoV-2-IN-21 (compound 10), a penicillin sulfone benzyl C6 derivative, is a potent SARS-CoV-2 main protease inhibitor, with an IC50 of 5.3 μM. SARS-CoV-2-IN-21 can be used for COVID-19 research.
  • 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-P4040
    Ac-D-DGla-LI-Cha-C

    HCV Protease Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. Ac-D-DGla-LI-Cha-C can be used for the research of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases.
  • HY-106560
    Proglumetacin

    SARS-CoV COX Inflammation/Immunology
    Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].
  • 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-N4155
    2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid

    HIV Protease HSV Cancer Infection
    2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells.
  • HY-144260
    3CPLro-IN-1

    SARS-CoV Infection
    3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive drug target for fighting COVID-19.
  • HY-N0554
    Escin IA

    HIV Protease Cancer Infection
    Escin IA is a triterpene saponin isolated from Aesculus hippocastanum, 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-114233
    MC-GGFG-Exatecan

    MC-GGFG-DX8951

    Drug-Linker Conjugates for ADC Cancer
    MC-GGFG-Exatecan (MC-GGFG-DX8951) is a drug-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC).
  • 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-15256
    Faldaprevir

    BI 201335

    HCV Protease Infection
    Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection.
  • HY-147850
    JMI-346

    Parasite Infection
    JMI-346 is a potent PfFP-2 (Plasmodium falciparum falcipain-2 protease) inhibitor. JMI-346 inhibits the growth of CQ S (3D7; IC50=13 µM) and CQ R (RKL-9; IC50=33 µM) strains of P. falciparum. JMI-346 has the potential to be used as an anti-malarial agent.
  • HY-B0372AS
    Bromhexine-d3 hydrochloride

    SARS-CoV Autophagy HIV Metabolic Disease
    Bromhexine-d3 (hydrochloride) is deuterium labeled Bromhexine (hydrochloride). 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-143422
    MALT1-IN-3

    MALT1 Cancer
    MALT1-IN-3 (compound 122) is a potent MALT1 protease inhibitor, with an IC50 of 0.06 μM. MALT1-IN-3 has IC50 of 0.14 and 0.13 μM for human IL6/IL10 in OCI-LY3 cells, respectively.
  • HY-10237S
    Boceprevir-d9

    EBP 520-d9; SCH 503034-d9

    HCV Protease HCV SARS-CoV Infection
    Boceprevir-d9 (EBP 520-d9) is the deuterium labeled Boceprevir. 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-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-124748A
    ENMD-1068 hydrochloride

    Protease Activated Receptor (PAR) Apoptosis Inflammation/Immunology
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.
  • HY-150600
    NS2B/NS3-IN-7

    Virus Protease Infection
    NS2B/NS3-IN-7 (compound 26) is a highly potent Zika virus NS2B-NS3 protease inhibitor with a Ki value of 2.33 nM. NS2B/NS3-IN-7 can reduce amounts of ZIKV-infected cells.
  • 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-144263
    3CPLro-IN-2

    SARS-CoV Infection
    3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive drug target for fighting COVID-19.
  • HY-10264B
    Edoxaban tosylate monohydrate

    DU-176b monohydrate

    Factor Xa Thrombin Cardiovascular Disease Cancer
    Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research.
  • HY-10264C
    Edoxaban hydrochloride

    DU-176 hydrochloride

    Factor Xa Thrombin Cardiovascular Disease
    Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research.
  • HY-N7073
    Silymarin

    SARS-CoV Cancer Infection Inflammation/Immunology Neurological Disease
    Silymarin is an extract of the milk thistle (Silybum marianum). Silymarin is an effective SARS-CoV-2 main protease (M pro) inhibitor. Silymarin can significantly reduce tumor cell proliferation, angiogenesis as well as insulin resistance. Silymarin has the chemopreventive effect on hepatocellular carcinoma (HCC). Silymarin has the potential for COVID-19 research.
  • HY-10264
    Edoxaban

    DU-176

    Factor Xa Thrombin Cardiovascular Disease Cancer
    Edoxaban (DU-176b) is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban can be used in preventing thromboembolic disease research.
  • HY-144062
    INSCoV-614(1B)

    SARS-CoV Infection
    INSCoV-614(1B) is a potent inhibitor of M pro (3CL pro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-614(1B) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1).
  • 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-10264A
    Edoxaban tosylate

    DU-176b

    Factor Xa Thrombin Cardiovascular Disease Cancer
    Edoxaban (DU-176b) tosylate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease research.
  • 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-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-150514
    ARN1468

    Others Infection
    ARN1468 (compound 5) is an orally active and potent serpins inhibitor. ARN1468 can inhibit serpins activity would set the protease free to further reduce prion accumulation. ARN1468 shows anti-prion effect in ScGT1 RML, ScGT1 22L, ScN2a RML, and ScN2a 22L cell lines, with EC50 values of 8.64, 19.3, 11.2, and 6.27 μM.
  • 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-144063
    INSCoV-600K(1)

    SARS-CoV Infection
    INSCoV-600K(1) is a potent inhibitor of M pro (3CL pro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-600K(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1).
  • HY-144061
    INSCoV-601I(1)

    SARS-CoV Infection
    INSCoV-601I(1) is a potent inhibitor of M pro (3CL pro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1).
  • HY-12594
    Paritaprevir

    ABT-450; Veruprevir

    HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) is a potent, orally active and antiviral 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. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor).
  • 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-114015
    APC-6860

    Ser/Thr Protease Cancer
    APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.
  • HY-106161S
    Rupintrivir-d4

    AG7088-d4

    Virus Protease Enterovirus Infection Inflammation/Immunology
    Rupintrivir-d4 (AG7088-d4) is the deuterium labeled Rupintrivir. 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-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-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-15275
    BMS-265246

    CDK Angiotensin-converting Enzyme (ACE) Cancer Infection
    BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.
  • 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-144833
    SARS-CoV-2 3CLpro-IN-1

    SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CL pro. 3CL pro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases.
  • HY-133894
    Bofutrelvir

    FB2001

    SARS-CoV Infection
    Bofutrelvir (FB2001) is a SARS-CoV-2 main protease M pro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077).
  • 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-120822
    Cyclotheonamide A

    Ser/Thr Protease Cardiovascular Disease
    Cyclotheonamide A is a serine protease inhibitor (cyclic polypeptide), which can be obtained from marine sponges of the genus Theonella. Cyclotheonamide A shows potent inhibitory activity against trypsin (Ki=0.023 µM) and streptokinase (Ki=0.035 µM) and moderate inhibitory activity against human α-thrombin (Ki=0.18 µM). Cyclotheonamide A can be used in study of antithrombotic.
  • HY-12594A
    Paritaprevir dihydrate

    ABT-450 dihydrate; Veruprevir dihydrate

    HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor).
  • HY-144645
    SP-471P

    Virus Protease DNA/RNA Synthesis Infection
    SP-471P is a potent dengue virus (DENV) protease inhibitor with EC50s of 5.9 μM, 1.4 μM, 5.1 μM and 1.7 μM for DENV1, DENV2, DENV3 and DENV4, respectively and CC50 value over 100 μM. SP-471P can reduce DENV viral RNA synthesis.
  • HY-149034
    Influenza A virus-IN-8

    S5

    Influenza Virus Infection
    Influenza A virus-IN-8 (S5) is a macrocyclic peptide with no cytotoxic. Influenza A virus-IN-8 is also a potent Influenza A Virus (IAV) inhibitor (with sufficient protease stability) with IC50s of 6.7 and 6.6 nM for H1 and H5 variants, respectively. Influenza A virus-IN-8 shows good affinitiescan to H1 variants, binds to a conserved region in the HA stem with a Kd of 1.0 nM.
  • HY-100604
    JNJ-40418677

    γ-secretase Amyloid-β Neurological Disease
    JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC50s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis NF-κB 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-142648A
    (R)-MLT-985

    MALT1 Cancer
    (R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor with an IC50 of 3 nM. (R)-MLT-985 has an IC50 of 20 nM for MALT1-dependent IL-2 production in Jurkat cells. (R)-MLT-985 suppresses growth and aberrant CARD11/BCL10/MALT1 complex signaling in ABC-DLBCL cells.
  • 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-N144101
    SARS-CoV MPro-IN-2

    SARS-CoV Infection
    SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M pro with an IC50 value of 72.07 nM. The main protease (M pro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in drug discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19.
  • HY-143423A
    (S)-MALT1-IN-5

    MALT1 Cancer Inflammation/Immunology
    (S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease. (S)-MALT1-IN-5 inhibits the activity of MALT1 is expected to be able to correct the enhancement of MALT1 activity due to abnormality of T cell receptor signal or B cell receptor signal, and cancer or inflammatory disease caused by MALT1 activity is expected. (S)-MALT1-IN-5 has the potential for the research of MALT1-related diseases (extracted from patent WO2020111087A1, compound 1).
  • 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-147849
    JMI-105

    Parasite Infection
    JMI-105 is a potent PfFP-2 (Plasmodium falciparum falcipain-2 protease) inhibitor. JMI-105 inhibits the growth of CQ S (3D7; IC50=8.8 µM) and CQ R (RKL-9; IC50=14.3 µM) strains of P. falciparum. JMI-105 significantly decreases parasitemia and prolonged host survival in a murine model with P. berghei ANKA infection. JMI-105 has the potential to be used as an anti-malarial agent.
  • 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.
  • HY-152005
    SARS-CoV-2 3CLpro-IN-6

    SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CL pro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19).
  • HY-112585
    Darunavir-d9

    TMC114-d9; UIC-94017-d9

    HIV HIV Protease Infection Inflammation/Immunology
    Darunavir-d9 (TMC114-d9) is the deuterium labeled Darunavir. 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-151901
    SARS-CoV-2 Mpro-IN-5

    SARS-CoV Infection
    SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM.
  • HY-151900
    SARS-CoV-2 Mpro-IN-4

    SARS-CoV Virus Protease Infection
    SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM.
  • HY-14993
    SCH79797

    Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 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 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-N0110
    Palmatine chloride

    Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.
  • HY-N0110A
    Palmatine

    Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Palmatine is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral 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-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-134851
    HIV-1 inhibitor-6

    HIV Infection
    HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to drugs targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM.
  • HY-151477
    SARS-CoV-2-IN-32

    SARS-CoV Cancer Infection
    SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19.
  • HY-146887
    USP7-IN-9

    Deubiquitinase Apoptosis Cancer
    USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21.
  • HY-151478
    SARS-CoV-2-IN-33

    SARS-CoV Cancer Infection
    SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19.
  • 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-N0110B
    Palmatine hydroxide

    Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.
  • 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-151535
    SARS-CoV-2 3CLpro-IN-5

    SARS-CoV Infection Inflammation/Immunology
    SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19).
  • HY-113953
    Z-Asp-CH2-DCB

    Caspase Apoptosis 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-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-N9725
    16-Hydroxycleroda-3,13-dien-15,16-olide

    16ξ-Hydroxycleroda-3,13-dien-15,16-olide

    Dipeptidyl Peptidase Metabolic Disease
    16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy.