Merck, 662107-25MG, UbcH13 Inhibitor, NSC697923

General description
A cell-permeable nitrofuran compound that selectively inhibits the E2 Ubiquitin-conjugating enzyme Ubc13- (Cat. No. 438075), but not UbcH5c-, catalyzed K63-linked polyUb chain formation by preventing Ubc13-Ub thioester bond formation. Effectively inhibits Ubc13-Uev1A (UBE2V1) E2 complex-mediated NF-κB activation, Ubc13-Mms2 (UBEV2) E2 complex-mediated DNA DSB (double-strand break) repair activation, as well as Ubc13-dependent p53 nuclear export in cultures (1 to 2 µM). The combined NF-κB inhibition and p53 activation via Ubc13 inhibition is shown to be particularly effective against the proliferation of ABC (Activated B-cell-like) and GCB (Germinal center B-cell-like) DLBCL (Diffuse Large B-Cell Lymphoma) cell lines and primary DLBCL cultures via apoptosis induction (1 to 2 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Ubc13
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Pulvino, M., et al. 2012. Blood 1668.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)