WM-8014 (Synonyms: WM8014,WM 8014) |
| カタログ番号GC18153 |
WM-8014 は、ヒストンアセチルトランスフェラーゼのメンバーである MOZ の阻害剤であり、IC50 は 55 nM です。
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Cas No.: 2055397-18-5
Sample solution is provided at 25 µL, 10mM.
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Target: lysine acetyltransferases, KAT6A(MOZ), KAT6B(MORF/QKF)
WM-8014 induces cell cycle exit and cellular senescence without causing DNA damage. Senescence is INK4A/ARF-dependent and is accompanied by changes in gene expression that are typical of loss of KAT6A function. WM-8014 potentiates oncogene-induced senescence in vitro and in a zebrafish model of hepatocellular carcinoma.
Data:
Treatment of MEFs with WM-8014 leads to cellular senescence.
Because KAT6A suppresses senescence, the ability of WM-8014 to induce cell cycle arrest is tested in embryonic day (E)14.5 mouse embryonic fibroblasts (MEFs). Cells treated with WM-8014 failed to proliferate after 10 days of treatment (IC50 2.4 μM).
(Left: effects of WM-8014 compared with the inactive compound WM-2474 or DMSO vehicle control on cell growth of MEFs grown in 3% O2. Right: effects of the dose of WM-8014 and the duration of treatment.)
Western blot of MEFs treated with increasing doses of WM-8014 and controls as indicated.
KD(KAT6A)=0.005μM KD(KAT5) = 0.9μM KD(KAT7) = 0.09 μM
References
1. Baell JB, et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257.
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