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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.

  • Marizomib
    T16012437742-34-2
    Marizomib (ML858) is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM, respectively.
    • $553
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  • Bortezomib
    T2399179324-69-7
    Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.
    • $48
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  • MG-132
    T2154133407-82-6
    MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.
    • $40
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  • Omarigliptin
    T23161226781-44-7
    Omarigliptin (MK-3102) has been used in trials studying the treatment of Type 2 Diabetes Mellitus and Chronic Renal Insufficiency.
    • $34
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  • Vildagliptin
    T1502274901-16-5
    Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine.
    • $39
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  • TCH-165
    T170111446350-60-2
    TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.
    • $68
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  • Sitagliptin
    T0242486460-32-6
    Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein/enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.
    • $36
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  • UK-101
    T132471000313-40-5In house
    UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM. UK-101 has a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer related diseases.
    • $410
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  • LXE408 fumarate
    T39214L
    LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.
    • $332
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  • Bortezomib-pinanediol
    T7854205393-22-2
    Bortezomib-pinanediol is a proteasome inhibitor. is a prodrug of Bortezomib.
    • $98
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  • Proteasome inhibitor IX
    T21854856849-35-9In house
    Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity(IC50 = 1.49 μM).
    • $32
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  • 1G244
    T14005847928-32-9In house
    1G244 is an inhibitor of DPP8/9 with antiatherosclerotic and antimyeloma properties. 1G244 had the IC50 values of 14 and 53 nM against DPP8 and DPP9, and The Ki values for 1G244 were 0.9 and 4.2 nM for DPP8 and DPP9
    • $33
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  • M3258
    T119242285330-15-4In house
    LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of immunoproteasome (LMP7).
    • $893
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  • Cilastatin
    T258382009-34-5
    Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.
    • $30
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  • Talabostat mesylate
    T4042150080-09-4
    Talabostat mesylate (PT100) is an orally active, selective inhibitor of dipeptidyl peptidases IV (DPP4, IC50: 0.18 nM), including tumor-associated fibroblast activation protein. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony-stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis.
    • $50
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  • MLN9708
    T20161201902-80-8
    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 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.
    • $43
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  • Calpeptin
    T6432117591-20-5
    Calpeptin is a potent, cell-permeable calpain inhibitor.
    • $30
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  • Oprozomib
    T6041935888-69-0
    Oprozomib (PR-047) (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 potential antineoplastic activity.
    • $58
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  • 18α-Glycyrrhetinic acid
    T27451449-05-4
    18α-Glycyrrhetinic acid (Enoxolone) is an inhibitor of NF-kB and an activator of the proteasome, and functions as a longevity-promoting and anti-aggregation factor in multicellular organisms. It induces apoptosis.
    • $42
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  • Delanzomib
    T6027847499-27-8
    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 peptidylglutamyl activities of the proteosome.
    • $43
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  • Tripterin
    T302834157-83-0
    Tripterin (Celastrol) is a natural product, a proteasome inhibitor that inhibits the pancreatic rennet-like activity of the 20S proteasome (IC50=2.5 μM). Tripterin has anti-inflammatory, anti-infectious, and immunomodulatory properties.
    • $46
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  • Aprotinin
    T33599087-70-1
    Aprotinin (Traskolan) a broad-spectrum serine protease inhibitor, inhibiting the activity of a number of different esterases and proteases, including trypsin, chymotrypsin, kallikrein, plasmin, tissue plasminogen activator, and tissue and leukocytic proteinases.
    • $39
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  • PI-1840
    T69411401223-22-0
    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) and postglutamyl-peptide-hydrolysis-like (PGPH-L).
    • $54
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  • Pepstatin
    T369526305-03-3
    Pepstatin (Pepsin Inhibitor S 735A) is a specific aspartic proteases inhibitor produced by actinomycetes, and inhibits the aspartic proteases cathepsin D, pepsin and renin.
    • $32
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  • Ixazomib
    T21221072833-77-2
    Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).
    • $41
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  • ONX-0914
    T6029960374-59-8
    ONX-0914 (PR-957) is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome.
    • $48
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  • ML604440
    T120791140517-08-3
    ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.
    • $135
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  • Carfilzomib
    T1795868540-17-4
    Carfilzomib (PR-171) is a proteasome inhibitor that irreversibly binds to the chymotrypsin of the 20S proteasome. Carfilzomib has antitumor activity and may be used to treat multiple myeloma.
    • $48
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  • Proteasome β2c/i-IN-1
    T813732322333-75-3
    Proteasome β2c/i-IN-1 (compound 37) serves as a selective inhibitor targeting the β2c and β2i subunits of the human proteasome [1].
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  • Aclacinomycin A hydrochloride
    T1023875443-99-1
    Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II.
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  • Proteasome-IN-5
    T813711613134-34-1
    Proteasome-IN-5, also known as compound 5, acts as a proteasome inhibitor [1].
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  • PR 39 (porcine) acetate
    TP1961L
    PR 39 (porcine) acetate is a noncompetitive, reversible and allosteric proteasome inhibitor. PR 39 (porcine) acetate reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway.
    • $197
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  • β5i-IN-1
    T80697
    β5i-IN-1 is a selective inhibitor of β5i, exhibiting potent activity with an IC50 of 8.463 nM. It modulates immune responses by promoting the release of TNF-α and IL-6 and affecting NF-κB transcriptional activity. This compound has applications in the research of idiopathic pulmonary fibrosis [1].
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  • Lactacystin
    T15702133343-34-7
    Lactacystin is an antibiotic Streptomyces spp. the metabolite and is an effective and selective proteasome inhibitor (IC50: 4.8 μM for 20S proteasome). Lactacystin inhibits cell growth and induces neurite outgrowth and also inhibits the lysosomal enzyme cathepsin A.
    • $88
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  • Z-Gly-Pro-Phe-Leu-CHO
    T80735159659-05-9
    Z-Gly-Pro-Phe-Leu-CHO (Z-GPFL-CHO) is a tetrapeptide aldehyde serving as a selective and potent proteasome inhibitor, demonstrating inhibition constants (Ki) of 1.5 µM, 2.3 µM, and 40.5 µM for branched-chain amino acid-preferred, small neutral amino acid-preferred, and chymotrypsin-like activities, respectively, and an inhibitory concentration (IC50) of 3.1 µM for peptidyl-glutamyl peptide hydrolyzing activity [1].
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  • LU-002i
    T819091838705-22-8
    LU-002i is a selective inhibitor targeting the human proteasome subunits β2c and β2i, demonstrating an inhibitory concentration (IC50) of 220 nM for β2i [1].
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  • Gabexate mesylate
    T037256974-61-9
    Gabexate mesylate (FOY) is a serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.
    • $51
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  • RAMB4
    T12579145888-79-5
    RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.
    • $76
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  • MUN57694
    T9090858557-69-4
    MUN57694 is an inhibitor of 26S proteasome.
    • $56
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  • Z-LLY-FMK
    T78632133410-84-1
    Z-LLY-FMK (Calpain Inhibitor IV) serves as an inhibitor of calpain, a family of proteases implicated in the apoptosis of various cell systems. Specifically, this compound suppresses intestinal cell apoptosis following common bile duct ligation [1].
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  • Trelagliptin succinate
    T22961029877-94-8
    Trelagliptin succinate (SYR-472 succinate) is a long-acting inhibitor of dipeptidyl peptidase-4 (DPP-4), being developed for the treatment of type 2 diabetes (T2D).
    • $39
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  • RA375
    T36902
    RA375, an inhibitor of RPN13 (26S proteasome regulatory subunit), enhances UPR signaling, ROS production, and apoptosis. Demonstrating ten times the efficacy against cancer lines compared to RA190, RA375 owes its increased activity to nitro ring substituents and the inclusion of a chloroacetamide warhead.
    • $35
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  • PR-924
    T165681416709-79-9
    PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.
    • $722
    5 days
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  • Trelagliptin
    T6237865759-25-7
    Trelagliptin (SYR-472) is a highly specific and long-acting DPP-4 inhibitor.
    • $41
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  • Z-Leu-Leu-Tyr-COCHO
    T80102204649-66-1
    Z-Leu-Leu-Tyr-COCHO is a potent inhibitor of chymotrypsin-like activity, exhibiting a Ki value of 3.0 nM [1].
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  • Z-Ala-Arg-Arg-AMC
    T7862590468-18-1
    Z-Ala-Arg-Arg-AMC (Fluorogenic Proteasome Substrate) serves as a fluorogenic substrate designed to assay the trypsin-like activity within the proteasome [1].
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  • AC-55541
    T2370916170-19-9
    AC-55541 (AOB2796) is a novel PAR2 agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.
    • $36
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  • Brensocatib
    TQ00381802148-05-5
    Brensocatib (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).
    • $67
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  • DD1
    T8978187585-11-1
    DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.
    • $163
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  • Alogliptin Benzoate
    T2401850649-62-6
    Alogliptin Benzoate (SYR 322)(SYR 322), an effective and specific DPP-4 inhibitor (IC50<10 nM), exhibits greater than 10, 000-fold selectivity over DPP-8/9. Alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines.
    • $43
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