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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mg/mL|
Evaluation of the in vitro growth-inhibitory effect of epoxomicin on Babesia parasites.
Aboulaila M, et al. Vet Parasitol. 2010 Jan 20;167(1):19-27. PMID: 19896277.
The proteasome inhibitor epoxomicin has potent Plasmodium falciparum gametocytocidal activity.
Czesny B, et al. Antimicrob Agents Chemother. 2009 Oct;53(10):4080-5. PMID: 19651911.
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses.
Schwarz K, et al. J Immunol. 2000 Jun 15;164(12):6147-57. PMID: 10843664.
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity.
Meng L, et al. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8. PMID: 10468620.
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