Size | Price | Stock |
---|---|---|
5mg | $144 | In-stock |
10mg | $230 | In-stock |
25mg | $410 | In-stock |
50mg | $615 | In-stock |
100mg | $920 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-100832 |
M.Wt: | 795.02 |
Formula: | C43H66N6O8 |
Purity: | >98 % |
Solubility: | DMSO : ≥ 27 mg/mL (33.96 mM) |
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. IC50 & Target: IC50: 66±1.2 nM (CBX7)[1] 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[1].
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