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Pathways Recommended: Metabolic Enzyme/Protease
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Protease selectivity

" in MedChemExpress (MCE) Product Catalog:

208

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15667
    P005091
    20+ Cited Publications

    P5091

    Deubiquitinase Cancer
    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
    P005091
  • HY-P0078
    TRAP-6
    5+ Cited Publications

    PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6

    Protease Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4 .
    TRAP-6
  • HY-108462
    ML-SA1
    5+ Cited Publications

    Dengue Virus TRP Channel Flavivirus 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 .
    ML-SA1
  • HY-10235
    Telaprevir
    40+ Cited Publications

    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 .
    Telaprevir
  • HY-14588
    Lopinavir
    15+ Cited Publications

    ABT-378

    HIV HIV Protease SARS-CoV Infection Neurological Disease Cancer
    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 .
    Lopinavir
  • HY-18236
    MDL-28170
    15+ Cited Publications

    Calpain Inhibitor III

    Proteasome Neurological Disease Inflammation/Immunology
    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 .
    MDL-28170
  • HY-10264
    Edoxaban
    5+ Cited Publications

    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 .
    Edoxaban
  • HY-117793
    I-191
    1 Publications Verification

    Protease Activated Receptor (PAR) Cancer
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist .
    I-191
  • HY-139399
    Safimaltib
    2 Publications Verification

    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 .
    Safimaltib
  • HY-153045
    BAY-805
    3 Publications Verification

    Deubiquitinase Cancer
    BAY-805, a chemical probe, is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .
    BAY-805
  • HY-116815
    Lalistat 1
    2 Publications Verification

    Beta-lactamase 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 .
    Lalistat 1
  • HY-10264B
    Edoxaban tosylate monohydrate
    5+ Cited Publications

    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 .
    Edoxaban tosylate monohydrate
  • HY-10264A
    Edoxaban tosylate
    5+ Cited Publications

    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 .
    Edoxaban tosylate
  • HY-121282
    Mepazine
    2 Publications Verification

    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 .
    Mepazine
  • HY-19837
    BMS-986120
    1 Publications Verification

    Protease Activated Receptor (PAR) Inflammation/Immunology
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
    BMS-986120
  • HY-125959
    Ucf-101
    1 Publications Verification

    Apoptosis Cardiovascular Disease Neurological 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 .
    Ucf-101
  • HY-128971
    LHVS
    3 Publications Verification

    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 .
    LHVS
  • HY-13487
    USP7/USP47 inhibitor
    3 Publications Verification

    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.
    USP7/USP47 inhibitor
  • HY-122700

    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 .
    Factor D inhibitor 6
  • HY-P2518

    Protease Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
    Protease-Activated Receptor-1, PAR-1 Agonist
  • HY-10300
    Narlaprevir
    5 Publications Verification

    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 .
    Narlaprevir
  • HY-16709
    USP7-IN-1
    5+ Cited Publications

    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.
    USP7-IN-1
  • HY-P4284

    Proteasome ClpP Bacterial Infection
    Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC50 of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC50 of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis .
    Z-GGF-CMK
  • HY-18200

    E5555; ER-172594-00

    Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .
    Atopaxar
  • HY-121282A
    Mepazine hydrochloride
    2 Publications Verification

    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 .
    Mepazine hydrochloride
  • HY-15256

    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 .
    Faldaprevir
  • HY-14351

    Protease Activated Receptor (PAR) Inflammation/Immunology
    AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5 .
    AC-264613
  • HY-112818

    Atg4 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 .
    S130
  • HY-152101

    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 .
    LY1
  • HY-150790

    Protease Activated Receptor (PAR) Cardiovascular Disease
    BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect .
    BMS-986141
  • HY-148072

    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 .
    MM3122
  • HY-163319

    ClpP Apoptosis Cancer
    NCA029 is a potent and selective homo sapiens caseinolytic protease P (HsClpP) activator with an EC50 of 0.15 μM. NCA029 acts on HsClpP to activate an ATF3-dependent integrative stress response, leading to colon cancer cell death .
    NCA029
  • HY-120528A
    GB-110 hydrochloride
    1 Publications Verification

    Protease Activated Receptor (PAR) Inflammation/Immunology Cancer
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM .
    GB-110 hydrochloride
  • HY-W790014

    Cathepsin Infection
    Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .
    Z-FG-NHO-BzOME
  • HY-19400

    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.
    DPC-681
  • HY-Y0241

    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 .
    2-Cyanopyrimidine
  • HY-112968

    APC Cardiovascular Disease
    Human Protein C is activated by α-thrombin or α-thrombin/thrombomodulin complex to a serine protease, namely activated protein C (APC). Human Protein C can selectively inactivate factors Va and VIIIa and is a potent anticoagulant .
    Human protein C
  • HY-P5062A

    Decanoyl-Arg-Val-Arg-Lys-chloromethylketone TFA

    Furin Infection
    DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
    DEC-RVRK-CMK TFA
  • HY-115753

    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) .
    Calpain Inhibitor-1
  • HY-112128
    USP7-IN-3
    1 Publications Verification

    Deubiquitinase MDM-2/p53 Cancer
    USP7-IN-3 (Compound 5) is an effective and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7). USP7-IN-3 can be used for research on acute lymphoblastic leukemia .
    USP7-IN-3
  • HY-120624

    Ser/Thr Protease Inflammation/Immunology
    BMS-354326 is a tryptase inhibitor with an IC50 of 1.8 nM. BMS-354326 exhibits excellent selectivity against trypsin and most other related serine proteases. BMS-354326 can be used in the research of asthma and inflammatory diseases .
    BMS-354326
  • HY-155556

    ClpP Cancer
    ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
    ZG36
  • HY-145349

    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).
    FXIa-IN-6
  • HY-P5062

    Decanoyl-Arg-Val-Arg-Lys-chloromethylketone

    Furin Infection
    DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
    DEC-RVRK-CMK
  • HY-122592

    Factor Xa Cardiovascular Disease
    Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research .
    Zifaxaban
  • HY-14853

    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 .
    Darexaban
  • HY-17367S4

    BMS-232632-d6

    Isotope-Labeled Compounds 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 .
    Atazanavir-d6
  • HY-158763

    TG0205221

    SARS-CoV Cathepsin Virus Protease Infection
    MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 can be used in clinical studies of COVID-19 .
    MPI8
  • HY-14360

    Cathepsin Metabolic Disease
    MK 1256 is a highly selective and orally active inhibitor of tissue protease K (Cat K) with an IC50 of 0.62 nM. MK 1256 shows extremely high selectivity towards other tissue proteases (all > 1100 times), with only a slightly lower selectivity for tissue protease F (Cat F) (110 times). MK 1256 exhibits strong anti-bone resorption activity in the osteoporosis model of rhesus monkeys with ovariectomy. MK 1256 can be used for research on osteoporosis .
    MK 1256
  • HY-174998

    HIV HIV Protease Infection
    HIV-1 protease-IN-15 (Compound 27) is an orally active and selective inhibitor targeting HIV-1 protease with a pIC50 value of 9.347. HIV-1 protease-IN-15 inhibits HIV protein maturation, blocks viral replication. HIV-1 protease-IN-15 is promising for research of HIV-1 infection .
    HIV-1 protease-IN-15

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