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WM-8014
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
WM-8014图片
CAS NO:2055397-18-5
规格:98%
分子量:384.42
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍

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).

WM-8014

(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.)

WM-8014

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

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.