Cat.No. | Name | Information |
---|---|---|
M1902 | MG132 | MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). |
M2071 | ONX-0914 | Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation. |
M1686 | Bortezomib (PS-341) | Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
M2193 | Epoxomicin | Epoxomicin is a cell-permeable, novel proteasome inhibitor with an IC50 value of 4 nM. |
M2035 | IU1 | IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM. |
M21515 | Zetomipzomib maleate | Zetomipzomib (KZR-616) maleate is a first-in-class inhibitor of immunoproteasome that selectively targets the immunoproteasome subunit LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50:131/179 nM=hLMP7/mLMP7). Potential of Zetomipzomib maleate for use in multiple autoimmune diseases. |
M21267 | LXE408 | LXE408 is an oral antileishmanarial compound that selectively targets the kinetoplastid proteosome vs. the mammalian proteosome. |
M21181 | Zetomipzomib | Zetomipzomib (KZR-616) is the first immunoproteasome inhibitor that selectively targets the immunoproteasome subunits LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7). Zetomipzomib has potential for use in a variety of autoimmune diseases. |
M20599 | PI-1840 | PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). |
M20398 | Ixazomib Citrate (MLN9708) | Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3. |
M14522 | Pepstatin Trifluoroacetate | 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. |
M14521 | Pepstatin Ammonium | 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. |
M14519 | ONX-0914 TFA | ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. |
M14518 | Marizomib | Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. |
M14517 | Capzimin | Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor. |
M14516 | Aclacinomycin A hydrochloride | 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. |
M13366 | (R)-MG-132 | (R)-MG-132 (Z-LEu-LEu-Al) is a cellular permeable proteasome and Calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively. |
M11459 | ML604440 | ML604440 is a potent, specific and cell-permeable inhibitor of the proteasome β 1I (LMP2) subunit. ML604440 disrupts MHC class I cell surface expression, IL-6 secretion and naive T helper differentiation to 17 T helper cells. ML604440 improves experimental colitis and EAE disease. |
M11402 | TCH-165 | Tch-165 is a small molecule modulator of proteasome assembly that increases 20S levels and promotes 20S-mediated protein degradation. |
M11294 | Alicapistat | Alicapistat (ABT-957) is an orally active, selective inhibitor of human calpains 1 and 2 that can be used in alzheimer's disease (AD) studies. |
M10767 | M-3258 | M3258 is an oral bioavailable, potent, reversible, and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 for LMP7 IC50 is 3.6 nM in cells IC50 3.4 nM. |
M9577 | RA190 hydrochloride | RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. |
M9570 | PTP1B-IN-9 | PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor with anticancer activity. |
M5221 | MG-101 | MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). IC50 value: 150 nM (Ki) |
M4985 | VR23 | VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM). |
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