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UNC3866

CAS No. : 1872382-47-2

產(chǎn)品活性：UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC₅₀=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

研究領(lǐng)域：Epigenetics

作用靶點：Histone Methyltransferase

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 K_d 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 K_d 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.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Peptidomimetic Library  |  Reprogramming Compound Library  |  Chemical Probe Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  Peptide Library  |  Membrane Protein-targeted Compound Library  |  PRMT5-IN-17  |  EZM0414  |  BIX-01294  |  WDR5-IN-5  |  PRMT5-IN-22  |  Gambogenic acid  |  SGC707  |  Dot1L-IN-7  |  MS1943  |  PRMT5-IN-21  |  NSD3-IN-3  |  DCLX069  |  MAK683  |  DS-437  |  EPZ020411  |  WDR5-IN-4 TFA  |  Amodiaquine dihydrochloride  |  Furamidine  |  SMYD3-IN-2  |  UNC0642  |  Chaetocin  |  UNC0646  |  UNC0224  |  EBI-2511  |  BVT948  |  MM-401  |  CMP-5  |  EPZ-719

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