WM-1119 |
| カタログ番号GC18154 |
WM-1119 は非常に強力で選択的な KAT6A 阻害剤であり、リンパ腫細胞における KAT6A の IC50 は 0.25 μM です。WM-1119 と KAT6A、KAT5、および KAT7 との結合 KD 値は、それぞれ 2 nM、2.2 μM、0.5 μM です。
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Cas No.: 2055397-28-7
Sample solution is provided at 25 µL, 10mM.
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Target: lysine acetyltransferases, KAT6A(MOZ), KAT6B(MORF/QKF)
WM-1119 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-1119, which has increased bioavailability, arrests the progression of lymphoma in mice
Data:
Treatment with WM-1119 arrests lymphoma growth.
Growth inhibition assays of Eμ-Myc lymphoma cell line EMRK1184 treated with WM-1119 and WM-8014 at the doses indicated.
KD(KAT6A)=0.002μM KD(KAT5) = 2.2μM KD(KAT7) = 0.5 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.
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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