A-395 is a potent and selective EED inhibitor. A-395 includes potent binding to EED with Ki = 0.4 nM, inhibits the PRC2 complex with IC50 = 34 nM for methylation of H3K27 and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, A-395 inhibits the PRC2 complex (thus inhibiting the formation of H3K27me3) with IC50 = 90 nM (RD rhabdoid tumor cell line; 3 days). A-395 represents a first-in-class antagonist of PRC2 protein-protein interactions (PPI) for use as a chemical probe to investigate the roles of EED-containing protein complexes.
MedKoo Cat#: 407490
Name: A-395 hydrochloride
CAS#: 2089148-72-9 (free base)
Chemical Formula: C26H38Cl3FN4O2S
Exact Mass: 486.2465
Molecular Weight: 596.02
Elemental Analysis: C, 52.39; H, 6.43; Cl, 17.84; F, 3.19; N, 9.40; O, 5.37; S, 5.38
The following data is based on the product molecular weight 596.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
