product name Epoxomicin
Description: Epoxomicin is a potent and selective proteasome inhibitor with anti-inflammatory activity, it 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. The novel α-epoxy ketone moiety of Epoxomicin forms covalent bonds with residues in particular catalytic subunits of the enzyme, disabling activity.
References: Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.
554.72
Formula
C28H50N4O7
CAS No.
134381-21-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (180.3 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (180.3 mM)
Solubility (In vivo)
Synonyms
BU-4061T
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | BALB/c mice |
| Formulation & Dosage | Dissolved in 10% DMSO/PBS; 2.9 mg/kg; i.p. injection |
| References | Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8. |
