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A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM[1].

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 nMinhibit the PRC2 complex with an IC50 value 34 nM for methylation of H3K27and 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 nMinhibiting the formation of H3K27me3. For characterization details of A-395please visit the A-395 probe summary on the Structural Genomics Consortium (SGC) website.

A-395N is the negative control for the active enantiomerA-395. A-395N is available from Sigma. To learn more about and purchase A-395N

[1] He Y, et al. The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat Chem Biol. 2017 Apr;13(4):389-395. DOI:10.1038/nchembio.2306