ALEXIS Biochemicals: Epoxomicin

ALX-350-254

Revised 10-Mar-08

Epoxomicin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Proteasome / Ubiquitin Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-254-C050		50 µg	132.00 USD

Product Specification

FORMULA:	C₂₈H₅₀N₄O₇
MW:	554.7
CAS NUMBER:	134381-21-8
MERCK INDEX:	14: 3630
SOURCE/HOST:	Synthetic.
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (15mg/ml); insoluble in water.
ACTIVITY:	k_obs/[I] = 25’000M^-1s^-1 versus 20S proteasome.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Avoid freeze/thaw cycles. Protect from light.
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin. Effectively inhibits NF-κB activation in vitro and potently blocks inflammation in vivo in the mouse ear edema assay.

Product Specific Literature References

Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. (Tokyo) 45, 1746 (1992) Abstract
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency: K.B. Kim, et al.; Bioorg. Med. Chem. Lett. 9, 3335 (1999) Abstract
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999) Abstract
Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology: N. Sin, et al.; Bioorg. Med. Chem. Lett. 9, 2283 (1999) Abstract
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses: K. Schwarz, et al.; J. Immunol. 164, 6147 (2000) Abstract
Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431: K. Ohkawa, et al.; Int. J. Oncol. 24, 425 (2004) Abstract

Further Categories Containing This Product:

Antitumor Agents (Enzyme Inhibitors) • Proteasome / Related Products • NF-kB Pathway Inhibitors • Anti-inflammatory Agents Other Products • Antibiotics for Inflammation Research • Antibiotics - NF-kB Inhibitors • Antitumor Antibiotics

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