Catalog No.S7038 Synonyms: BU-4061T,Aids010837
Molecular Weight(MW): 554.72
Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.
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|Description||Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.|
|Features||Epoxomicin is a natural product isolated from an Actinomycetes species.|
Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome. Epoxomicin (100 nM) results in a 30-fold increase in the levels of p53 protein, a known target of the proteasome, in HUVECs. Epoxomicin (10 μM) results in the accumulation of ubiquitinated proteins in HeLa cells. Epoxomicin (10 μM) inhibits IκBα degradation by 10-fold in HeLa cells. Epoxomicin (10 μM) produces a significant dose-dependent reduction in TNF-α-stimulated NF-κB DNA-binding activity in HeLa cells.  Epoxomicin inhibits proliferating of EL4 lymphoma cells with biotinylated chimerae with IC50 of 4 nM.  Epoxomicin (1 μM) leads to a reduction of LCMV GP33 presentation and an enhancement of GP276 presentation.  Epoxomicin inhibits growth of Babesia bigemina with IC50 of 4 nM. Epoxomicin (0.5 mg/kg and 0.05 mg/kg) results in peak parasitemia levels of 34.8% and 42.3% in B. microti.  Epoxomicin (100 nM) decreases the total parasitemia by 78%, 86% and 77% in Plasmodium falciparum. Epoxomicin (10 μM) inhibits gametogenesis and exflagellation as well as development into oocysts of anopheles mosquitoes. 
|In vivo||Epoxomicin (0.58 mg/kg per day) reduces the CS response by 44% relative to the control group of mice treated with vehicle alone. Epoxomicin (2.9 mg/kg) potently inhibits the irritant-associated inflammatory response by 95% when ear edema measurements are made 24 hours postchallenge in mice. |
-  Meng L, et al. Proc Natl Acad Sci U S A, 1999, 96(18), 10403-10408.
-  Kim KB, et al. Bioorg Med Chem Lett, 1999, 9(23), 3335-3340.
-  Schwarz K, et al. J Immunol, 2000, 164(12), 6147-6157.
|In vitro||DMSO||100 mg/mL (180.27 mM)|
|Ethanol||100 mg/mL (180.27 mM)|
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