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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.

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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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, respectively. UK-101 exhibits 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.
  • $239
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aprotinin
T33599087-70-1
Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.
  • $39
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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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Epoxomicin
T6830134381-21-8
Epoxomicin (BU-4061T,Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.
  • $127
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Pepstatin
T369526305-03-3
Pepstatin (Pepsin Inhibitor S 735A) is an aspartate protease inhibitor that also inhibits HIV protease activity with specific and oral activity. Pepstatin inhibits autophagy.
  • $32
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ONX-0914
T6029960374-59-8
ONX-0914 (PR-957) is a potent and highly specific immunoproteasome inhibitor with minimal cross-reactivity to the constitutive proteasome.
  • $48
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Puromycin aminonucleoside
T1668458-60-6
Puromycin aminonucleoside (NSC-3056) increases podocyte permeability by modulating ZO-1 in an oxidative stress-dependent manner.
  • $39
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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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Saikogenin A
T168385092-09-1
Saikogenin A is a dipeptidyl peptidase-4 inhibitor.
  • $198
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Linagliptin
T0191668270-12-0
Linagliptin (BI 1356) is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.
  • $38
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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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(R)-MG-132
T126281211877-36-9
(R)-MG-132 (Z-Leu-D-leu-leu-al) is the enantiomer of MG-132.
  • $34
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Marizomib
T16012437742-34-2
Marizomib 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.[3]
  • $123
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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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K-7174 dihydrochloride
T11742L191089-60-8
K-7174 dihydrochloride is a proteasome and GATA inhibitor that inhibits neuronal degeneration and induces apoptosis.
  • $30
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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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Tomatine
T378617406-45-0
Tomatine (lycopersicin) is an antiproliferatve agent of breast adenocarcinoma cells.
  • $30
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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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Gly-Pro-pNA hydrochloride
T36583103213-34-9
Gly-Pro-pNA hydrochloride (Gly-Pro p-nitroanilide hydrochloride) is a dipeptidyl peptidase inhibitor that inhibits dipeptidyl peptidase II, dipeptidyl peptidase IV and dipeptidyl peptidase IX.
  • $34
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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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3-Feruloylquinic acid
TN12621899-29-2
3-O-Feruloylquinic acid is a protease inhibitor, it exerts moderate inhibitory effect against AIV (H5N1) in vitro.
  • $215
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Calpeptin
T6432117591-20-5
Calpeptin is a potent, cell-permeable calpain inhibitor.
  • $30
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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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