Biological Activity
A-395 is a potent and selective chemical probe for the polycomb protein EED (embryonic ectoderm development), an essential component of Polycomb repressive complex 2 (PRC2), involved in transcriptional repression through methylation of histone H3K27. A-395 has been found to bind to EED in vitro with a Ki value of 0.4 nM, inhibit the PRC2 complex with an IC50 value 34 nM for methylation of H3K27, and have >100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In RD rhabdoid tumor cell line A-395 inhibited the PRC2 complex with an IC50 value of 90 nM, inhibiting the formation of H3K27me3. For characterization details of A-395, please visit the
A-395 probe summary on the Structural Genomics Consortium (SGC) website.
A-395N is the negative control for the active enantiomer, A-395. A-395N is available from Sigma. To learn more about and purchase A-395N,
click here.
To learn about other SGC chemical probes for epigenetic targets, visit
sigma.com/sgc
