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UNC3866 is a potent antagonist of CBX4 and CBX7 chromodomains with a Kd of ~100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains. UNC3866 antagonizes the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. [1]

UNC3866 is the most potent ligand reported for CBX7, with a Kd of 97 ± 2.4 nM. UNC3866 antagonizes the CBX7-H3 interaction, assayed by AlphaScreen (IC50 = 66 ± 1.2 nM). Affinity of UNC3866 for CBX2, CBX4, CBX6 and CBX8 is surprisingly well associated with the percent sequence identity of each chromodomain relative to that of CBX7. UNC3866 is equally potent for CBX4, which is most similar to CBX7, whereas it is 18-, 6- and 12-fold

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