Search Result
Results for "
Cathepsin L Inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W790014
-
|
Cathepsin
|
Infection
|
Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .
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-
-
- HY-115733
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(Rac)-Z-Phe-Phe-FMK
|
Cathepsin
|
Cancer
|
Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor .
|
-
-
- HY-P4306
-
-
-
- HY-P10117
-
-
-
- HY-P10118
-
|
Cathepsin
|
Others
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Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.
|
-
-
- HY-15100
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AAE581
|
Cathepsin
|
Inflammation/Immunology
|
Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis .
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-
-
- HY-50887
-
|
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 .
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-
-
- HY-P10061
-
|
Cathepsin
|
Cancer
|
Cathepsin K inhibitor 4 is a potent carbohydrazide Cathepsin K inhibitor with IC50s of 13 nM, 269 nM, 296 nM for human, rat, mouse Cathepsin K, respectively .
|
-
-
- HY-137392
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1-Naphthalenesulfonyl-Ile-Trp-CHO
|
Cathepsin
|
Others
|
Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations .
|
-
-
- HY-103351
-
-
-
- HY-U00377
-
-
-
- HY-151524
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies .
|
-
-
- HY-143714
-
|
Cathepsin
|
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-15958
-
VBY-825
1 Publications Verification
|
Cathepsin
|
Cancer
|
VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
|
-
-
- HY-10042
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MK-0822
|
Cathepsin
|
Metabolic Disease
Cancer
|
Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
|
-
-
- HY-146985
-
|
Cathepsin
|
Neurological Disease
Cancer
|
Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic .
|
-
-
- HY-152204
-
|
Cathepsin
|
Cancer
|
Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC50s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells .
|
-
-
- HY-146581
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively .
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-
-
- HY-146580
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively .
|
-
-
- HY-102087
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JPM-OEt
3 Publications Verification
|
Cathepsin
|
Cancer
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
|
-
-
- HY-103352
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L-235
|
Cathepsin
|
Metabolic Disease
|
L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .
|
-
-
- HY-146584
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity .
|
-
-
- HY-112583
-
|
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-144813
-
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
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-156655A
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STI-1558 sodium
|
SARS-CoV
Cathepsin
|
Infection
|
Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
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-
-
- HY-P10065
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-
-
- HY-144812
-
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
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 .
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-
-
- HY-124202
-
|
Cathepsin
|
Others
|
SQ 32602 is an inhibitor of cathepsin E, with the IC50 of 88 nM .
|
-
-
- HY-P5999
-
-
-
- HY-N4289
-
|
Cathepsin
|
Cancer
|
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B .
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-
-
- HY-100231
-
|
|
|
Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively .
|
-
-
- HY-155611
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin C-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsin C with anti-inflammatory activity. Cathepsin C-IN-6 inhibts activation of neutrophil elastase,exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.,chronic obstructive pulmonary disease) .
|
-
-
- HY-103350
-
-
-
- HY-N10109
-
|
SARS-CoV
|
Infection
|
Gallinamide A is a potent inhibitor of cathepsin L with an IC50 value of 17.6 pM.
|
-
-
- HY-W796158
-
-
-
- HY-114374
-
|
Cathepsin
|
Inflammation/Immunology
|
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis .
|
-
-
- HY-18964
-
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-123531
-
|
Cathepsin
|
Inflammation/Immunology
|
JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a Ki value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation .
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-
-
- HY-15958A
-
|
Others
|
Cancer
|
(S,R,R)-VBY-825 is the isomer of VBY-825 (HY-15958), and can be used as an experimental control. VBY-825 is a novel reversible inhibitor of cathepsin with high inhibition of cathepsin B, L, S and V.
|
-
-
- HY-120709
-
-
-
- HY-103353
-
|
Cathepsin
Parasite
|
Infection
Cancer
|
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-163206
-
|
Cathepsin
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-77 (compound 11e) is a cathepsin L and cathepsin S inhibitor with Ki values of 111 nM and 103 nM, respectively. SARS-CoV-2-IN-77 inhibits SARS-CoV-2 with an EC50 value of 38.4 nM in Calu-3 cells without showing cytotoxicity .
|
-
-
- HY-103353A
-
|
Cathepsin
Parasite
|
Infection
Cancer
|
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows no inhibitory activity against cathepsin G .
|
-
-
- HY-109069
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-
-
- HY-128140
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-
-
- HY-161244
-
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
FGA145 is a dual, selective inhibitor for M pro and human Cathepsin L, with Kis of 3.71 μM, 9.82 μM and 53 nM, for Mal-M pro, pET21-M pro and Cathepsin L, respectively. FGA145 reveals a multitarget effects in the antiviral activity .
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-
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- HY-115454
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-
-
- HY-115454A
-
|
Cathepsin
|
Others
|
GB111-NH2 hydrochloride is a cysteine cathepsin inhibitor, and can be used for cancer study .
|
-
-
- HY-P3012
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin G acts as a potent agonist of human platelet activation leading to their aggregation., and can be used for screening of relevant inhibitors .
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-
-
- HY-161245
-
|
Virus Protease
Cathepsin
|
Infection
|
FGA146 is a dual, selective inhibitor for M pro and human Cathepsin L, with Kis of 2.19 μM, 0.96 μM and 0.87 μM, for Mal-M pro, pET21-M pro and Cathepsin L, respectively. FGA146 reveals an antiviral activity against SARS-CoV-2 .
|
-
- HY-100223
-
|
|
|
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-123753
-
|
Cathepsin
|
Inflammation/Immunology
|
MDL 27399 is an inhibitor of human neutrophil cathepsin G (Ki = 7 μM). MDL 27399 can be used for research of inflammatory diseases .
|
-
- HY-10294
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SB-462795
|
Cathepsin
|
Metabolic Disease
Cancer
|
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-100350
-
CA-074Me
|
Cathepsin
|
Neurological Disease
Cancer
|
CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
|
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- HY-P3042
-
|
Cathepsin
|
Inflammation/Immunology
|
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research .
|
-
- 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 .
|
-
- HY-112318A
-
|
Cathepsin
|
Inflammation/Immunology
|
GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis .
|
-
- HY-118355
-
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-136888
-
Elastase Inhibitor III
|
Elastase
Cathepsin
|
Others
|
MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .
|
-
- HY-119293
-
K777
1 Publications Verification
|
Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Cancer
|
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-108044
-
|
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-112318
-
|
Cathepsin
|
Inflammation/Immunology
|
GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis .
|
-
- HY-P1081
-
|
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-122161
-
RWJ-355871
|
Cathepsin
|
Inflammation/Immunology
|
JNJ-10311795 (RWJ-355871), a potent dual inhibitor of neutrophil cathepsin G (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM), exhibits noteworthy antiinflammatory activity .
|
-
- HY-128971
-
|
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-15533
-
Z-FL-COCHO
|
Cathepsin
|
Inflammation/Immunology
|
LY 3000328 (Z-FL-COCHO) 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-P1081A
-
|
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-100227
-
E 64c
2 Publications Verification
|
|
|
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-163389
-
|
SARS-CoV
Cathepsin
|
Infection
|
Mpro/Cathepsin L-IN-1 (Compound 4d) is a SARS-CoV-2 M pro/hCatL inhibitor, with Kis of 5.54 μM and 0.701 μM respectively .
|
-
- HY-118762
-
|
Cathepsin
|
Cancer
|
KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM . KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines .
|
-
- HY-N2905
-
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-138208
-
|
Cathepsin
SARS-CoV
|
Infection
|
Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection .
|
-
- HY-N10109A
-
|
SARS-CoV
Parasite
Cathepsin
|
Infection
|
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
|
-
- HY-10290
-
|
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-126988
-
α-MAPI
|
Elastase
|
Others
|
SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .
|
-
- HY-162148
-
|
EGFR
|
Cancer
|
HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
|
-
- HY-112786
-
Vc-MMAF
|
Drug-Linker Conjugates for ADC
|
Cancer
|
MC-Val-Cit-PAB-MMAF (Vc-MMAF) is a agent-linker conjugate for ADC by using the tubulin inhibitor, MMAF, linked via cathepsin cleavable MC-Val-Cit-PAB. MC-Val-Cit-PAB-MMAF shows antitumor activity .
|
-
- HY-129116
-
|
SARS-CoV
Cathepsin
|
Infection
|
SSAA09E1 is a cathepsin L blocker (IC50: 5.33 μM).SSAA09E1 inhibits stages of viral entry. SSAA09E1 can be used for SARS-CoV infection research
|
-
- HY-141867
-
Z-Phe-Phe-FMK
|
Cathepsin
|
Neurological Disease
|
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
|
-
- HY-152108
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
|
-
- HY-152210
-
|
Cathepsin
|
Cancer
|
ASPER-29 is Asperphenamate HY-129578 analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC50 value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer .
|
-
- HY-124322
-
|
Beta-secretase
|
Neurological Disease
Inflammation/Immunology
|
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-157477
-
|
SARS-CoV
Cathepsin
|
Infection
|
SARS-CoV-2 3CLpro-IN-22 (Compound 17) is a cathepsin L (CTSL ) inhibitor with an IC50 value of 32.5 nM. SARS-CoV-2 3CLpro-IN-22 can be used for the study of SARS-CoV-2 virus .
|
-
- HY-P4532
-
|
Cathepsin
|
Neurological Disease
|
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II .
|
-
- HY-P0111
-
Z-WE(OMe)HD(OMe)-FMK
|
Caspase
Cathepsin
|
Cancer
|
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
|
-
- HY-116171
-
|
Proteasome
|
Cardiovascular Disease
Neurological Disease
|
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury .
|
-
- HY-15652
-
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-P0109A
-
(1S)-Z-FA-FMK
|
SARS-CoV
Cathepsin
Apoptosis
Caspase
|
Infection
Cancer
|
Z-FA-FMK ((1S)-Z-FA-FMK) is a potent Cathepsin B and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host .
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-
- HY-P0109
-
|
|
|
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position .
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-
- HY-15652A
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ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
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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-16594
-
|
Proteasome
Apoptosis
ROS Kinase
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Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
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- HY-19269
-
|
|
|
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 .
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-
- HY-10472
-
|
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
-
|
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 .
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-
- HY-13240A
-
|
Beta-secretase
|
Neurological Disease
|
LY2886721 hydrochloride 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 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
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-
- HY-151900
-
|
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 .
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-
- HY-151901
-
|
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 .
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-
- HY-13438
-
|
Beta-secretase
|
Cancer
|
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
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- HY-W744699
-
(+)-Larixol
|
Src
ERK
Akt
|
Inflammation/Immunology
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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-
- HY-W745090
-
|
Formyl Peptide Receptor (FPR)
Src
ERK
Akt
p38 MAPK
|
Others
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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-
-
-
HY-L012
-
|
4475 compounds
|
Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.
MCE designs a unique collection of 4475 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.
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Cat. No. |
Product Name |
Type |
-
- HY-W745090
-
|
Biochemical Assay Reagents
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W790014
-
|
Cathepsin
|
Infection
|
Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .
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-
- HY-P4306
-
-
- HY-P10117
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-
- HY-P10118
-
|
Cathepsin
|
Others
|
Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.
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-
- HY-P10061
-
|
Cathepsin
|
Cancer
|
Cathepsin K inhibitor 4 is a potent carbohydrazide Cathepsin K inhibitor with IC50s of 13 nM, 269 nM, 296 nM for human, rat, mouse Cathepsin K, respectively .
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-
- HY-137392
-
1-Naphthalenesulfonyl-Ile-Trp-CHO
|
Cathepsin
|
Others
|
Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations .
|
-
- HY-P10065
-
-
- HY-P5999
-
-
- HY-W796158
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-
- HY-P3012
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin G acts as a potent agonist of human platelet activation leading to their aggregation., and can be used for screening of relevant inhibitors .
|
-
- HY-P3042
-
|
Cathepsin
|
Inflammation/Immunology
|
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research .
|
-
- HY-136888
-
Elastase Inhibitor III
|
Elastase
Cathepsin
|
Others
|
MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor. MeOSuc-AAPV-CMK also inhibits cathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .
|
-
- HY-P1081
-
|
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-P1081A
-
|
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-141867
-
Z-Phe-Phe-FMK
|
Cathepsin
|
Neurological Disease
|
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
|
-
- HY-P4532
-
|
Cathepsin
|
Neurological Disease
|
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II .
|
-
- HY-P0111
-
Z-WE(OMe)HD(OMe)-FMK
|
Caspase
Cathepsin
|
Cancer
|
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N4289
-
-
-
- HY-N2905
-
-
-
- HY-N10109A
-
-
-
- HY-16594
-
|
Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
|
Proteasome
Apoptosis
ROS Kinase
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
-
- HY-N10109
-
-
-
- HY-W744699
-
(+)-Larixol
|
Larix decidua Miller
Structural Classification
Natural Products
Pinaceae
Source classification
Plants
|
Src
ERK
Akt
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-149926
-
|
|
Alkynes
|
Cathepsin Inhibitor 3 (Compound 53k) is a non-radioactive intermediate in compound [ 18F] 2k radioactive synthesis, which has selectivity for cathepsin S. Cathepsin Inhibitor 3 can undergo radioactive fluorination and can be used for fluorine-18 labeling research . Cathepsin Inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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