MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis[1][2][3].
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.
Suc-Gly-Gly-Phe-pNA is the chymotrypsin substrate with an Km value of 1.6 mM[1][2].
UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2].
Ac-ANW-AMC is a fluorogenic substrate for immunoproteasome. Ac-ANW-AMC can be used to measure β5i activity (Ex=345 nm, Em=445 nm)[1][2].
MG-262 is a reversible proteasome inhibitor with diverse biological activities[1][2][3].
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research[1].
Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
Z-Leu-Leu-Glu-AMC is a substrate peptide, and can be used for determination of postacidic-like hydrolysing activity of 20S proteasome[1]
BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells[1][2].
Z-Leu-Tyr-Chloromethylketone is a calpain inhibitor[1].
Z-LLF-CHO (Z-Leu-Leu-Phe-CHO) is a potent inhibitor of the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex (Ki = 460 nM). Z-LLF-CHO is also a NF-κB nuclear translocation inhibitor[1][2].
A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM); shows weak activity toward LMP2 and no detectable activity toward β1, β2, or MECL1.
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD)[1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM[2].
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity[1][2].
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[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
Isovalerylcarnitine chloride, a product of the catabolism of L-leucine, is a potent activator of the Ca2+-dependent proteinase (calpain) of human neutrophils[1].
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1][2].
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M[1].
Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i[1].
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans[1][2][3].
cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration[1][2]. MDL-28170 also block γ-secretase[4].
A-933548 is a potent Calpain inhibitor. A-933548 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.
KZR-616 maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases[1][2].
Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC50=100 nM; Ki=2.89 μM)[1].
Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets[1]. Calpeptin is also an inhibitor of cathepsin K[2].
Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.