包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Kinase experiment: | For SMYD2 inhibition, 10 μL of BAY-598 or DMSO is first incubated with recombinant SMYD2 in methylation buffer reaction for 1 h at 30℃, and then 2 μCi of 3H-AdoMet is added to the mix and incubated overnight at 30℃. The reaction mixture is resolved by SDS-PAGE followed by autoradiography, Coomassie stain, or MS analysis[1]. |
Cell experiment: | Cells are seeded in 96-well plates at 2000 cells per well (optimum density for growth) in a total volume of 100 μL of medium containing 2% fetal bovine serum. Serially diluted BAY-598 in 100 μL of medium is added to the cells 12 h later. After 72 h of incubation, cell viability is assessed by an MTT assay according to the manufacturer's instructions[1]. |
文献引用 | |
产品描述 | 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. References [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. |