| Cat.No. | Name | Information |
|---|---|---|
| M3884 | Celastrol | 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 (BU-4061T) is a cell-permeable, selective and irreversible proteasome inhibitor with an IC50 value of 4 nM. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. |
| 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). MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132 is also a calpain inhibitor with IC50 of 1.2 μM. |
| M1686 | Bortezomib (PS-341) | Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
| M66250 | MV151 | MV151 is a cell-permeable, fluorescent, broad-spectrum proteasome inhibitor that specifically targets all active subunits of the proteasome and immunoproteasome in living cells and can be used to label the proteasome in vitro and in vivo. |
| M59302 | BT317 | BT317 is a blood-brain transmissible mitochondrial Lon peptidase I (LonP1) and CT-L proteasome inhibitor. BT317 can increase the production of reactive oxygen species (ROS) and induce apoptosis in astrocytoma cells. BT317 has antitumor activity. |
| 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. |
| M27794 | ALLM | ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI). |
| 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. |
| 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. |
| 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 | RAMB4 | RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor with anticancer activity. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. |
| M7764 | PD150606 | PD150606 is a selective, cellular permeable non-peptide calpain inhibitor with Ki of 0.21 μ m and 0.37 μ m on μ-calpains and M-calpains, respectively, and has neuroprotective 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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