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Proteases/Proteasome Proteasome

Proteasome

Proteasomes are protein complexes which degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that help such reactions are called proteases.Proteasomes are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins.
Cat No. product name
T1176 Racecadotril Racecadotril has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.
T1795 Carfilzomib Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma.
T2016 Ixazomib Citrate MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 is ML...
T2122 Ixazomib MLN2238, a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (I...
T2154 MG-132HOT MG-132 is a potent cell-permeable 20S proteasome inhibitor (IC50: 100 nM). It also inhibits calpain (IC50: 1.2 μM).
T2370 AOB2796 AOB2796 is a novel PAR2 agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assa...
T2399 BortezomibHOT Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay).
T2583 Cilastatin Cilastatin is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which re...
T3028 Celastrol Celastrol is an effective proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome(IC50=2.5 μM) with antioxidant and anti-inflammat...
T3359 Aprotinin Aprotinin a broad-spectrum serine protease inhibitor, inhibiting the activity of a number of different esterases and proteases, including trypsin, chymotrypsin...
T4467 UAMC 00039 dihydrochloride UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
T6027 Delanzomib CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome (IC50: 3.8 nM). It only marginally inhibits the tryptic and peptidylglut...
T6029 ONX-0914 ONX-0914 is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome.
T6041 Oprozomib Oprozomib (ONX 0912) ,an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has ...
T6830 Epoxomicin Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH c...
T6941 PI-1840 PI-1840( IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor,with little proteasome proteolytic effects on trypsin-like (T-L) an...
T6999 Teneligliptin hydrobromide Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP...
T7016 VR23 VR23 is a potent proteasome inhibitor. Data shows IC50 =1 nM for trypsin-like proteasomes, IC50=50-100 nM for chymotrypsin-like proteasomes, and IC50=3 μM fo...
TQ0038 AZD7986 AZD7986 is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).
T7854 Bortezomib-pinanediol Bortezomib-pinanediol is a proteasome inhibitor. is a prodrug of Bortezomib.
T7814 Alloxan monohydrate Alloxan monohydrate is a proteasome inhibitor
T8397 Ixazomib citrate Ixazomib citrate is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (IC50 of 3.4 nM ) with potentia...
TN1262 3-O-Feruloylquinic acid 3-O-Feruloylquinic acid is a protease inhibitor, it exerts moderate inhibitory effect against AIV (H5N1) in vitro.
T12561 Proteasome-IN-1 Proteasome-IN-1 is an inhibitor of proteasome.
T10061 (1S,2S)-Bortezomib (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S pro...
T10238 Aclacinomycin A hydrochloride Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (...
T12628 (R)-MG-132 (R)-MG-132 is the enantiomer of MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
T13858 RA190 RA190 inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
T12579 PTP1B-IN-9 PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.
T15678 KZR-504 KZR-504 is of interest for the treatment of autoimmune disease. KZR-504 is a selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2) (IC...
T15702 Lactacystin Lactacystin is an antibiotic Streptomyces spp. the metabolite and is an effective and selective proteasome inhibitor (IC50: 4.8 μM for 20S proteasome). Lactacy...
T16568 PR-924 PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multip...
T11924 LMP7-IN-1 LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of im...
Racecadotril
T1176CAS 81110-73-8
Racecadotril has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.
Carfilzomib
T1795CAS 868540-17-4
Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma.
Ixazomib Citrate
T2016CAS 1201902-80-8
MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 is ML...
Ixazomib
T2122CAS 1072833-77-2
MLN2238, a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (I...
MG-132 HOT
T2154CAS 133407-82-6
MG-132 is a potent cell-permeable 20S proteasome inhibitor (IC50: 100 nM). It also inhibits calpain (IC50: 1.2 μM).
AOB2796
T2370CAS 916170-19-9
AOB2796 is a novel PAR2 agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assa...
Bortezomib HOT
T2399CAS 179324-69-7
Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay).
Cilastatin
T2583CAS 82009-34-5
Cilastatin is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which re...
Celastrol
T3028CAS 34157-83-0
Celastrol is an effective proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome(IC50=2.5 μM) with antioxidant and anti-inflammat...
Aprotinin
T3359CAS 9087-70-1
Aprotinin a broad-spectrum serine protease inhibitor, inhibiting the activity of a number of different esterases and proteases, including trypsin, chymotrypsin...
UAMC 00039 dihydrochloride
T4467CAS 697797-51-6
UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
Delanzomib
T6027CAS 847499-27-8
CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome (IC50: 3.8 nM). It only marginally inhibits the tryptic and peptidylglut...
ONX-0914
T6029CAS 960374-59-8
ONX-0914 is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome.
Oprozomib
T6041CAS 935888-69-0
Oprozomib (ONX 0912) ,an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has ...
Epoxomicin
T6830CAS 134381-21-8
Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH c...
PI-1840
T6941CAS 1401223-22-0
PI-1840( IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor,with little proteasome proteolytic effects on trypsin-like (T-L) an...
Teneligliptin hydrobromide
T6999CAS 906093-29-6
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP...
VR23
T7016CAS 1624602-30-7
VR23 is a potent proteasome inhibitor. Data shows IC50 =1 nM for trypsin-like proteasomes, IC50=50-100 nM for chymotrypsin-like proteasomes, and IC50=3 μM fo...
AZD7986
TQ0038CAS 1802148-05-5
AZD7986 is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).
Bortezomib-pinanediol
T7854CAS 205393-22-2
Bortezomib-pinanediol is a proteasome inhibitor. is a prodrug of Bortezomib.
Alloxan monohydrate
T7814CAS 2244-11-3
Alloxan monohydrate is a proteasome inhibitor
Ixazomib citrate
T8397CAS 1239908-20-3
Ixazomib citrate is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (IC50 of 3.4 nM ) with potentia...
3-O-Feruloylquinic acid
TN1262CAS 1899-29-2
3-O-Feruloylquinic acid is a protease inhibitor, it exerts moderate inhibitory effect against AIV (H5N1) in vitro.
Proteasome-IN-1
T12561CAS 374080-21-4
Proteasome-IN-1 is an inhibitor of proteasome.
(1S,2S)-Bortezomib
T10061CAS 1132709-14-8
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S pro...
Aclacinomycin A hydrochloride
T10238CAS 75443-99-1
Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (...
(R)-MG-132
T12628CAS 1211877-36-9
(R)-MG-132 is the enantiomer of MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
RA190
T13858CAS 1617495-03-0
RA190 inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
PTP1B-IN-9
T12579CAS 145888-79-5
PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.
KZR-504
T15678CAS 1629052-78-3
KZR-504 is of interest for the treatment of autoimmune disease. KZR-504 is a selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2) (IC...
Lactacystin
T15702CAS 133343-34-7
Lactacystin is an antibiotic Streptomyces spp. the metabolite and is an effective and selective proteasome inhibitor (IC50: 4.8 μM for 20S proteasome). Lactacy...
PR-924
T16568CAS 1416709-79-9
PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multip...
LMP7-IN-1
T11924CAS 2285330-15-4
LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of im...