A-196是有效的选择性SUV420H1和SUV420H2化学抑制剂,在多种细胞系中抑制H4K20me二甲基化和三甲基化。
Cas No. | 1982372-88-2 |
Canonical SMILES | ClC1=C(Cl)C=C(C(C2=CC=NC=C2)=NN=C3NC4CCCC4)C3=C1 |
分子式 | C18H16Cl2N4 |
分子量 | 359.25 |
溶解度 | DMSO : ≥ 31 mg/mL (86.29 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. Target: A-196 is a selective chemical probe for SUV420H1/H2. A-196 is the first potent and selective chemical probe for SUV420H1 and SUV420H2. The in vitro activity of A-196 includes inhibition of SUV420H1 with IC50 = 25 nM and SUV420H2 with IC50 = 144 nM for methylation of H4K20me and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cell assays, A-196 inhibits the di- and tri-methylation of H4K20me in multiple cell lines with IC50< 1 μM. SUV420H1 and SUV420H2 are two highly homologous methyltransferases that di- and tri-methylate 'Lys-20' of histone H4. |