Ubiquitin E1 Inhibitor, UBEI-41(PYR-41)

Ubiquitin-mediated proteolysis is an important pathway of non-lysosomal protein degradation that controls the timed destruction of a number of cellular regulatory proteins including p53. In mammalian cells, there are more than 30 different E2s and hundreds of E3s but only one essential E1. Therefore, E1 is the single common step in the ubiquitination process. While proteasome inhibitor prevents the degradative function of ubiquitination, E1 inhibitor blocks both degradative and non-degradative functions of ubiquitination and thus is a valuable tool for exploring the biological roles of ubiquitination and other components in ubiquitination pathway.

At we offer the first generation of ubiquitin E1 inhibitor designated UBEI-41.

Properties:
UBEI-41 is a cell-permeable ubiquitin E1 inhibitor with an IC50 ~ 5 µM. It inhibits the degradation of many proteins and also prevents cytokine-induced alpha-kappa B phosphorylation and EGF-induced receptor ubiquitination.

Chemical Name:
4[4-(5-Nitro-furan-2-ylmethylene)-3,4-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester.

Chemical Structure:

Purity: 98%

Molecular Weight: 371

Catalog ID: UBEI-41

Other Information:
$185/vial/50uL, containing 50 mM UBEI-41 in DMSO solution and suggested concentration of 1 – 50 µM for in vitro experiments and 5 -50 µM for cellular experiments. Store at dark, -20°C. For MSDS, please click here to download.

References:
1. Yili Yang, Jirouta Kitagaki,Ren-Ming Dai,Yien Che Tsai,Kevin L. Lorick,Robert L. Ludwig,Shervon A. Pierre, Jane P. Jensen, Ilia V. Davydov, Pankaj Oberoi,Chou-Chi H. Li,John H. Kenten, John A. Beutler, Karen H. Vousden,and Allan M. Weissman. Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of PotentialCancer Therapeutics. Cancer Res. 67:(19) 9472-9481 October 2007

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