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. Author manuscript; available in PMC: 2016 Apr 20.
Published in final edited form as: Angew Chem Int Ed Engl. 2015 Feb 27;54(17):5166–5170. doi: 10.1002/anie.201412154

Figure 2.

Figure 2

SGC707 is a potent, selective, and non-competitive inhibitor of PRMT3. A) IC50 determination for SGC707 (●) and XY1 (○) was performed at balanced condition (Km of both substrates). B) SPR studies confirmed that SGC707 had a high binding affinity to PRMT3 (KD = 85 ± 1 nm (n = 3)). C) Effect of SGC707 on the activity of 27 protein methyltransferases as well as DNMT1, DNMT3A-3L, DNMT3B-3L, and BCDIN3D (an RNA-methyltransfer- ase) were assessed at 1 (red), 5 (green), and 20 μm (purple) of compound and no inhibition was observed. No change in IC50 values at varying D) SAM or E) peptide concentrations was consistent with a noncompetitive pattern, confirming the allosteric mode of inhibition.