NSC697923 | E2 ubiquitin-conjugating enzyme inhibitor

NSC69723 (343351-67-7) is a selective inhibitor of the E2 ubiquitin-conjugating enzyme, Ubc13-Uev1A. Does not inhibit UbcH5c activity. Impedes the formation of the Ubc13 and inhibits NF-κB activation in activated B cell-like diffuse large B-cell lymphoma (ABC-DLBCL) cells.¹ Blocks proliferation and survival of both ABC-DLBCL and germinal center B cell-like (GCB)-DLBCL cell lines, and survival of primary DLBCL cells. NSC69723 acts via covalent bonding to E2 active site thiol.^2,3 Induces neuroblastoma cell death via activation of p53 and JNK.⁴

References/Citations:

1) Pulvino et al. (2012), Inhibition of proliferation and survival of diffuse large B-cell lymphoma cells by a small-molecule inhibitor of the ubiquitin-conjugating enzyme Ubc13-Uev1A; Blood, 120 1668
2) Strickson et al. (2013), The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signaling network by targeting the ubiquitin system; Biochem. J., 451 427
3) Hodge et al. (2015), Covalent Inhibition of Ubc13 Affects Ubiquitin Signaling and Reveals Active Site Elements Important for Targeting; ACS Chem. Biol., 10 1718
4) Cheng et al. (2014), A small-molecule inhibitor of UBE2N induces neuroblastoma cell death via activation of p53 and JNK pathways; Cell Death Dis., 5 e1079