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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-WM-8014
WM-8014

Chemical Structure : WM-8014

CAS No.: 2055397-18-5

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WM-8014 (WM8014;WM 8014)

货号: PC-35579Not For Human Use, Lab Use Only.

WM-8014 (WM8014) is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with Kd of 5 nM and IC50 of 8 nM.

规格 价格 库存 数量
10 mg ￥1980 In stock
25 mg ￥2980 In stock
50 mg ￥4980 In stock
100 mg ￥7980 In stock
200 mg Get quote
1 g Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
WM-8014 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.
WM-8014 selectively reduces liver volume in a zebrafish model of KRASG12V-driven hepatocellular overproliferation, robustly upregulate the cell cycle regulators Cdkn2a and Cdkn1a in hepatocytes.

物理化学性质&存储条件

分子量 384.425
分子式 C20H17FN2O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Baell JB, et al. Nature. 2018 Aug;560(7717):253-257.

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