Inhibitor for KAT6A (MOZ) and KAT6B (MORF/QKF), anticancer
CAS：2055397-18-5
分子式：C20H17FN2O3S
分子量：384.42
纯度：98%
存储：Store at -20°C

Background:

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 (IC₅₀2.4 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.

K_D(KAT6A)=0.005μM K_D(KAT5) = 0.9μM K_D(KAT7) = 0.09 μM

参考文献：

1. Baell JB, et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257.