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Beschreibung

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-kappaB activation (Effective Conc. = 2 µ,M 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 µ,M in U2OS cells), as well as Ubc13-dependent p53 nuclear export (Effective Conc.1 to 2 µ,M in OCI-Ly10 cells), but not Ubc13-independent NF-kappaB activation following TNF-alpha receptor stimulation. The combined NF-kappaB 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 µ,M)., 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-kappaB 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 µ,M). The combined NF-kappaB 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 µ,M).