Proteasome

ONX-0914 (PR-957) is a specific inhibitor of the immunoproteasome subunits low molecular weight polypeptide 7 (LMP7) and low molecular weight polypeptide 2 (LMP2), with IC 50 values of 0.34μM and 0.0057μM, respectively.

A 20S proteasome inhibitor and an active metabolite of MLN9708

A selective inhibitor of the 20S proteasome

inhibitor of the trypsin-like activity of the 20S proteasome

An inhibitor of calpains

Gliotoxin, an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi, is a specific inhibitor of 20S proteasomal chymotrypsin activity with an IC 50 of 10μM.

Bortezomib (PS-341), as a dipeptide boronic acid proteasome inhibitor with antitumor activity, can potently inhibiit 20S proteasome with Ki of 0.6 nM by targeting a threonine residue.

FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM.

KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively.

Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.

RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.

Alicapistat (ABT-957) (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD).

LMP7-IN-1 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. LMP7-IN-1 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. LMP7-IN-1 shows strong antitumor efficacy in multiple myeloma xenograft models. LMP7-IN-1 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), 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. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.

Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively.

Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively.

Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.

TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.

Calpain Inhibitor II (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases.

(R)-MG132 is a proteasome inhibitor with an IC 50 of 100 nM.