BRD4770 (Synonyms: HMTase Inhibitor VI) |
Catalog No.GC10259 |
BRD4770 es un inhibidor de la histona metiltransferasa G9a. BRD4770 reduce la dimetilaciÓn y la trimetilaciÓn de la lisina 9 en la histona H3 (H3K9) con una CE50 de 5 μM y tiene un efecto menor o menor hacia H3K27me3, H3K36me3, H3K4me3 y H3K79me3. BRD4770 puede activar la vÍa mutada de ataxia telangiectasia (ATM) e inducir la senescencia celular.
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Cas No.: 1374601-40-7
Sample solution is provided at 25 µL, 10mM.
BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).IC50 value: 5 uM (PANC-1 cell) [1]Target: G9a inhibitorBRD4770 activates the ATM pathway without inducing DNA damage, while the ATR pathway is not affected. BRD4770 is a novel probe for studying G9a and its role in cellular senescence.Treatment of 5 μM BRD4770 for 24 h decreased H3K9 trimethylation level by 23% in PANC-1 cells. BRD9539 also inhibits PRC2 activity.
References:
[1]. Yuan Y, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.
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