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Targets Recommended: Cathepsin

Results for "A2e cathepsin Inhibitors" in MCE Product Catalog:

59

Inhibitors & Agonists

1

Screening Libraries

4

Peptides

5

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-U00377
    Cathepsin Inhibitor 2

    Cathepsin Cancer Inflammation/Immunology
    Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.
  • HY-102087
    JPM-OEt

    Cathepsin Cancer
    JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
  • HY-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-112318
    GSK-2793660

    Cathepsin Inflammation/Immunology
    GSK-2793660 is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.
  • HY-111456
    DBCO-NHCO-PEG4-NHS ester

    ADC Linker Cancer
    DBCO-NHCO-PEG4-NHS ester ester is a MMP-2- and cathepsin B- (CatB) cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-N2905
    Aurantiamide acetate

    Asperglaucide

    Cathepsin Inflammation/Immunology
    Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of  inflammatory diseases.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-P0111
    Z-WEHD-FMK

    Caspase Cathepsin Cancer
    Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.
  • HY-50887
    L-873724

    Cathepsin Metabolic Disease
    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
  • HY-10042
    Odanacatib

    MK-0822

    Cathepsin Metabolic Disease
    Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
  • HY-15958
    VBY-825

    Cathepsin Cancer
    VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
  • HY-18234A
    Leupeptin hemisulfate

    Cathepsin Inflammation/Immunology
    Leupeptin hemisulfate is a membrane-permeable thiolprotease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion. Leupeptin hemisulfate also exhibits anti-inflammatory effect.
  • HY-112583
    MIV-247

    Cathepsin Neurological Disease
    MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
  • HY-18964
    MG-101

    Calpain inhibitor I; Ac-LLnL-CHO; ALLN

    Proteasome Cancer
    MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
  • HY-15100
    Balicatib

    AAE581

    Cathepsin Inflammation/Immunology
    Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
  • HY-N4289
    3-Epiursolic Acid

    Cathepsin Cancer
    3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B.
  • HY-103350
    CA-074

    Cathepsin Neurological Disease Cancer
    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
  • HY-109069
    Petesicatib

    Cathepsin Inflammation/Immunology
    Petesicatib is a cathepsin S inhibitor, used in research of immune diseases.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-112688
    H-Arg-4MβNA

    Others Others
    H-Arg-4MβNA is a substrate for cathepsin H, used for the detection of enzyme activity in gel electrophoresis.
  • HY-103353
    SID 26681509

    Cathepsin Parasite Cancer Infection
    SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
  • HY-20336
    Mc-Val-Cit-PABC-PNP

    Maleimidocaproyl-L-valine-L-citrulline-p-aminobenzyl alcohol p-nitrophenyl carbonate

    ADC Linker Cancer
    Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-129362
    Phe-Lys(Fmoc)-PAB

    ADC Linker Cancer
    Phe-Lys(Fmoc)-PAB is a cathepsin cleavable ADC linker used for the antibody-drug conjugates (ADCs).
  • HY-129349
    Phe-Lys(Trt)-PAB

    ADC Linker Cancer
    Phe-Lys(Trt)-PAB is a cathepsin cleavable ADC linker used for the antibody-drug conjugates (ADCs).
  • HY-78738
    MC-Val-Cit-PAB

    ADC Linker Cancer
    MC-Val-Cit-PAB is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate.
  • HY-100350
    CA-074 methyl ester

    CA-074Me

    Cathepsin Neurological Disease
    CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
  • HY-10294
    Relacatib

    SB-462795

    Cathepsin Cancer Metabolic Disease
    Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
  • HY-108044
    ONO-5334

    Cathepsin SARS-CoV Metabolic Disease
    ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-100223
    Calpeptin

    Cathepsin Proteasome Apoptosis Inflammation/Immunology
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
  • HY-15533
    LY 3000328

    Cathepsin Inflammation/Immunology
    LY 3000328 is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.
  • HY-W010347
    L-Homocysteine

    Endogenous Metabolite Inflammation/Immunology
    L-Homocysteine, a homocysteine metabolite, is a homocysteine that has L configuration. L-Homocysteine induces upregulation of cathepsin V that mediates vascular endothelial inflammation in hyperhomocysteinaemia.
  • HY-P1081
    Acetyl-Calpastatin(184-210)(human)

    Proteasome Inflammation/Immunology
    Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.
  • 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-112786
    MC-Val-Cit-PAB-MMAF

    Drug-Linker Conjugates for ADC Microtubule/Tubulin Cancer
    MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC with antitumor activity by using the tubulin inhibitor, MMAF, linked via cathepsin cleavable MC-Val-Cit-PAB.
  • HY-P1081A
    Acetyl-Calpastatin(184-210)(human) TFA

    Proteasome Inflammation/Immunology
    Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 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-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-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-10290
    MK-0674

    Cathepsin Metabolic Disease
    MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S.
  • HY-16594
    Lactacystin

    Proteasome Neurological Disease
    Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
  • 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-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-116171
    (Rac)-Calpain Inhibitor XII

    Proteasome
    (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
  • 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-13240
    LY2886721

    Beta-secretase Neurological Disease
    LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
  • 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-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-19269
    FK706

    Elastase Inflammation/Immunology
    FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.