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Epoxomicin (BU 4061T) is a naturally occurring selective proteasome inhibitor with anti-inflammatory activity. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome. Epoxomicin (BU 4061T) inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM. Epoxomicin also effectively inhibits NF-kappaB activation in vitro and potently blocks in vivo inflammation in the murine ear edema assay. In contrast to peptide aldehyde proteasome inhibitors, epoxomicin does not inhibit nonproteasomal proteases such trypsin, chymotrypsin, papain, calpain, and cathepsin B at concentrations of up to 50 microM. Treatment of proliferating cells with epoxomicin results in cell death through accumulation of ubiquinated proteins.
Arch Virol. 2021 Aug;166(8):2173-2185.
Interplay of the ubiquitin proteasome system and the innate immune response is essential for the replication of infectious bronchitis virus
Epoxomicin purchased from AbMole
Mol Cell. 2020 Nov 19;80(4):607-620.e12.
Paradoxical Mitophagy Regulation by PINK1 and TUFm
Epoxomicin purchased from AbMole
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Source | Mol Cell (2020), Figure 4, Epoxomicin (Abmole Bioscience Inc.) |
| Method | Cell Culture | |
| Cell Lines | HeLa and HEK293T cell lines | |
| Concentrations | 100 µM | |
| Incubation Time | 2-12 hours | |
| Results | CCCP treatment induced accumulation of mitochondrion-localized fulllength PINK1 protein and an enhanced p-S222-TUFm signal;applying the proteasome inhibitor MG132 or epoxomicin elevated cytosolic and mitochondrial cleaved PINK1 and the p-S222-TUFm signal, and so did the autophagosome formation inhibitors CK636 and Baf-A1, but to a lesser extent |
| Molecular Weight | 554.72 |
| Formula | C28H50N4O7 |
| CAS Number | 134381-21-8 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Proteasome Products |
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| Bortezomib (PS-341)
Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
| CTP-518
CTP-518 is a novel HIV protease inhibitor. CTP-518 has the potential to be the first HIV protease inhibitor toeliminate the need to co-dose with a boosting agent. |
| ITMN-191
ITMN-191 (Danoprevir, RG7227) is a potent and orally active inhibitor of hepatitis C virus (HCV) NS3/4A serine protease with an IC50 of 1.6 nM. |
| 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. |
| IU1
IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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