Potent and selective SMYD2 inhibitor
CAS：1906919-67-2
分子式：C22H20Cl2F2N6O3
分子量：523.4
纯度：98%
存储：Store at -20°C

Background:

BAY-598 is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), a lysine methyl transferase inhibitor that dimethylates histone H3K36 and methylates histone H3K4. SMYD2 also methylates Lys-370 of p53, leading to decreased DNA-binding activity. SMYD2 is over-expressed in several cancers with poor prognosis. BAY-598 inhibits?in vitro?methylation of p53K370 with an IC₅₀?value of 27 nM and in cells with an IC₅₀?value < 1 μM. BAY-598 is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.

参考文献

[1]. Reynoird N, et al. Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreaticcancer. Genes Dev. 2016 Apr 1;30(7):772-85.