UNC3866

Research use only, not for human use.

A potent, selective PRC1 chromodomains antagonist that binds to CBX4 and CBX7 with Kd of 100 nM.

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.

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.

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UNC 3866 | UNC-3866

Chromatin/Epigenetic

HMTase

CBX7-H3

Cancer

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1872382-47-2

795.0195

C43H66N6O8

>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

L-Serine, N-[4-(1,1-dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-, methyl ester

(-20℃)

With Ice Pack

≥ 2 years