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. 2012 Apr 26;7(7):1152–1157. doi: 10.1021/cb300139y

Figure 1.

Figure 1

Small-molecule inhibitors of G9a. (A) Classification of existing histone methyltransferases inhibitors (HMTi). Representative substrate- and cofactor-competitive HMTi’s are shown. (B) Synthetic chemistry scheme yielding 117 benzimidazoles as potential SAM mimetics for competitive inhibition of HMTs. (C) Chemical structures of BRD4770 and BRD9539. (D) Biochemical activities of G9a, PRC2, SUV39H1, NSD2, and DNMT1 following treatment with indicated concentrations of BRD9539. Data represent the mean and standard error of four independent reactions.