(R)-BAY-598 is an inhibitor of the lysine N-methyltransferase SMYD2 (IC50 = 1.7 μM) and a less active enantiomer of (S)-BAY-598 .1 It is selective for SMYD2 over proteinase-activated receptor 1 (PAR1; IC50 = >30 μM).
|1. Eggert, E., Hillig, R.C., Koehr, S., et al. Discovery and characterization of a highly potent and selective aminopyrazoline-based in vivo probe (BAY-598) for the protein lysine methyltransferase SMYD2. J. Med. Chem. 59(10), 4578-4600 (2016).