WM-8014

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WM-8014 (WM8014) 是一种高效、选择性的赖氨酸乙酰转移酶 KAT6A 抑制剂，Kd 为 5 nM，IC50 为 8 nM。

WM-8014 (WM8014) is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with Kd of 5 nM and IC50 of 8 nM; WM-8014 is reversible competitor of acetyl coenzyme A and inhibits MYST-catalysed histone acetylation, also inhibits closely related KAT6B (IC50=28 nM), displays >10-fold selectivity over KAT7 and KAT5 (IC50=342 nM and 224 nM), shows no inhibition against KAT8, KAT2A, KAT2B, KAT3A and KAT3B; induces cell cycle exit and cellular senescence without causing DNA damage, reduces acetylation of specific histone lysine residues and changes in gene expression that resemble the genetic loss of KAT6A; selectively reduces liver volume in a zebrafish model of KRASG12V-driven hepatocellular overproliferation, robustly upregulate the cell cycle regulators Cdkn2a and Cdkn1a in hepatocytes.(In Vitro):WM-8014 (Compound 36) is an inhibitor of MOZ, with an IC50 of 55 nM. WM-8014 causes cell senescence and suppresses the proliferation with IC50s of 1.6 μM and 551 nM, respectively. WM-8014 also reduces mRNA coding for the MOZ gene Cdc6 by 65.1%.

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WM8014 | WM 8014

Chromatin/Epigenetic

HAT

MOZ

Cancer

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2055397-18-5

384.425

C20H17FN2O3S

>98% (HPLC)

DMSO: ≥250 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(C1=CC(C2=CC=CC=C2)=CC(C)=C1F)NNS(=O)(C3=CC=CC=C3)=O

[1,1'-Biphenyl]-3-carboxylic acid, 4-fluoro-5-methyl-, 2-(phenylsulfonyl)hydrazide

(-20℃)

With Ice Pack

≥ 2 years