| Cat.No. | Name | Information |
|---|---|---|
| M3884 | Celastrol (Tripterin) | Celastrol (Tripterin) is a potent antioxidant and anti-inflammatory agent, as well as a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. |
| M2193 | Epoxomicin | Epoxomicin is a cell-permeable, novel proteasome inhibitor with an IC50 value of 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. |
| M2035 | IU1 | IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM. |
| M1902 | MG132 | MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). |
| M1686 | Bortezomib (PS-341) | Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
| M28190 | MG-115 | 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. |
| 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. |
| 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. |
| M18197 | 18alpha-Glycyrrhetinic acid | 18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1). |
| 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. |
| M14517 | Capzimin | Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor. |
| 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. |
| M11402 | TCH-165 | Tch-165 is a small molecule modulator of proteasome assembly that increases 20S levels and promotes 20S-mediated protein degradation. |
| 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). |
| M3478 | Gabexate Mesylate | Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation. |
| M3476 | CEP-18770 | CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome. |
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