UNC3866 is an inhibitor of chromobox homolog 7 (CBX7; Kd = 97 nM). It also binds to CBX4 (Kd = 94 nM) but is greater than 6-fold selective over CBX2, 6, and 8 and the chromodomain Y family (CDY) chromodomains CDY1, L1b, and L2 (Kds = 0.61-6.3 μM). UNC3866 pretreatment (30 μM) of PC3 lysates completely inhibits chemiprecipitation of CBX7. It induces a senescent-like morphology and reduces growth of PC3 cells with an EC50 value of 7.6 μM.
Polycomb group proteins (CBX4, CBX7) regulate cell fate decisions during embryogenesis. N-?[4-?(1,?1-Dimethylethyl)?benzoyl]?-?L-?phenylalanyl-?L-?alanyl-?L-?leucyl-?N6,?N6-?diethyl-?L-?lysyl-?L-serine Methyl Ester is a selective antagonist of CBX4 and CBX7 chromodomains. It also inhibits prostate cell proliferation.
