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. 2022 Jul 27;32:100823. doi: 10.1016/j.neo.2022.100823

Figure 1.

Figure 1

SOMCL-19-133 demonstrates potent and selective inhibition of NAE. (a) Chemical structures of MLN4924 and SOMCL-19-133. (b and c) Dose-response curves of enzymatic inhibition by SOMCL-19-133. (b) NAE; (c) UAE. NAE inhibitor MLN4924 and UAE inhibitor MLN7243 were used as the positive control, respectively. Data are represented as mean ± SD from three independent experiments. S133 is short for SOMCL-19-133. (d) Representative western blot analysis showing the effect of SOMCL-19-133 on Ubc12NEDD8, UBC10Ub, and Ubc9SUMO thioester levels. HCT-116 cells were treated with different concentrations of SOMCL-19-133 and MLN4924 for 4 h. Cell lysates were separated by non-reducing SDS-PAGE and immunoblotted using the indicated antibodies. The experiment was repeated three times. (e) Kinase affinity assay of SOMCL-19-133 against 468 kinases and some of their mutants at 1 µM with DiscoveRx KINOMEScan screening platform and presented as a TREEspot interaction map.