A-196 |
| カタログ番号GC32861 |
A-196 は、SUV420H1 および SUV420H2 の強力かつ選択的な阻害剤であり、IC50 値はそれぞれ 25 nM および 144 nM です。 A-196 は、基質競合的に SUV4-20 を生化学的に阻害します。 A-196 は、ゲノムの完全性におけるヒストンメチルトランスフェラーゼの役割を調査するための SUV4-20 のクラス初の化学プローブです。
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Cas No.: 1982372-88-2
Sample solution is provided at 25 µL, 10mM.
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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.
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