A highly potent, selective KAT6A/B inhibitor
CAS：2055397-28-7
分子式：C18H13F2N3O3S
分子量：389.38
纯度：98%
存储：Store at -20°C

Background:

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

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.