Biochem/physiol Actions

Primary TargetUbc13

Cell permeable: yes

General description

A cell-permeable nitro-tosylfuran compound that selectively inhibits the E2 Ubiquitin-conjugating enzyme Ubc13- (Cat. No. 662103), 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 (Effective Conc. = 2 µM in HEK293T, MEF, RAW264.7, and SUDHL-6 cultures), Ubc13-Mms2 (UBEV2) E2 complex-mediated DNA DSB (double-strand break) repair activation (Effective Conc. = 1 µM in U2OS cells), as well as Ubc13-dependent p53 nuclear export (Effective Conc.1 to 2 µM in OCI-Ly10 cells), but not Ubc13-independent NF-κB activation following TNF-α receptor stimulation. The combined NF-κB and p53 activation via Ubc13 inhibition is shown to be particularly effective against the proliferation of ABC (Activated B-cell-like; OCI-Ly3, OCI-Ly10) and GCB (Germinal center B-cell-like; OCI-Ly7, SUDHL-6) DLBCL (Diffuse Large B-Cell Lymphoma) lines, as well as primary DLBCL cultures, via apoptosis induction (Effective Conc.1 to 2 µM).

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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Pulvino, M., et al. 2012. Blood 1668.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)