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Epoxomicin

Chemical Structure : Epoxomicin

CAS No.: 134381-21-8

Epoxomicin (BU-4061T)

Catalog No.: PC-21916Not For Human Use, Lab Use Only.

Epoxomicin (BU-4061T) is a potent, selective and irreversible proteasome inhibitor, covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Epoxomicin (BU-4061T) is a potent, selective and irreversible proteasome inhibitor, covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity.
Epoxomicin does not inhibit nonproteasomal proteases such trypsin, chymotrypsin, papain, calpain, and cathepsin B at concentrations of up to 50 uM.
Epoxomicin is a more potent inhibitor of the chymotrypsin-like activity than lactacystin and the peptide vinyl sulfone NLVS.
Epoxomicin also effectively inhibits NF-kappaB activation in vitro and potently blocks in vivo inflammation in the murine ear edema assay.

Physicochemical Properties

M.Wt 554.73
Formula C28H50N4O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,3S)-N-((2S,3R)-3-Hydroxy-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxobutan-2-yl)-3-methyl-2-((2S,3S)-3-methyl-2-(N-methylacetamido)pentanamido)pentanamide

References

1. Hanada M, et al. J Antibiot (Tokyo). 1992 Nov;45(11):1746-52.

2. Meng L, et al. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.

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