UNC3866

A potent, selective PRC1 chromodomains antagonist that binds to CBX4 and CBX7 with Kd of 100 nM; displays 6- to 18-fold selectivity versus other CBX (CBX2/6/8) and CDY chromodomains, highly selectivity versus >250 other taergets in a Kme reader panel; inhibits PC3 cell proliferation with EC50 of 340 nM. (In Vitro) :UNC3866, a potent antagonist of the methyl-lysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently with a Kd of 100 nM for each, and is 6- to 18-fold selective versus seven other CBX and CDY chromodomains while being highly selective versus >250 other protein targets. UNC3866 inhibits PC3 cell proliferation, a known CBX7 phenotype, while UNC4219, a methylated negative control compound, has negligible effects. UNC3866 is a potent and cellularly active antagonist of PRC1 chromodomains. UNC3866 is the most potent ligand reported for CBX7 with a Kd of 97±2.4 nM. UNC3866 is equipotent for CBX4, which is most similar to CBX7, while it is 18-, 6- and 12-fold selective for CBX4/7 over CBX2, -6 and -8, respectively. Additionally, UNC3866 is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2.

1872382-47-2

UNC 3866 | UNC-3866

>98% (HPLC)

DMSO: ≥ 27 mg/mL

CC (C) (C) C1=CC=C (C (N[C@@H] (CC2=CC=CC=C2) C (N[C@@H] (C) C (N[C@@H] (CC (C) C) C (N[C@@H] (CCCCN (CC) CC) C (N[C@@H] (CO) C (OC) =O) =O) =O) =O) =O) =O) C=C1

C43H66N6O8

795.0195

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.