GlpBio

WM-80143X 积分

目录号: GC18153纯度: >99.50%同义词: WM8014,WM 8014
An inhibitor of KAT6A and KAT6B
WM-8014
Cas No.: 2055397-18-5
规格价格库存数量操作
5mg¥2,625.00现货
1
25mg¥5,250.00现货
1
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产品描述 Description

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 (IC50 2.4 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

References      

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

实验参考方法 Experimental Reference Method

Kinase experiment:

To determine the inhibition of Moz activity by the test compounds, assay reactions are conducted in a volume of 8 μL in 384-well low volume assay plates. The reactions are performed in assay buffer (100 mM Tris-HCl, pH 7.8, 15 mM NaCl, 1 mM EDTA, 0.01% Tween-20, 1 mM Dithiothreitol, and 0.02% m/v chicken egg white albumin). Reactions are set up with 0.4 μM Acetyl coenzyme A (AcCoA), 50 nM N-terminal histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRKV-GGK-biotin), 10 nM MOZ enzyme, and an acetyl-lysine specific antibody (final dilution 1: 10000). 11-point dilution series of the compounds (WM-8014) of the invention are prepared in DMSO; a volume of 100 nL is transferred using a pin tool into assay plates containing substrates, before adding enzyme to start the reaction. Positive (no compound) and negative (AcCoA omitted) control reactions are included on the same plates and receive the same amount of DMSO as the compound treated wells. After adding all reagents, the plates are sealed with adhesive seals and incubated for 90 minutes at room temperature[1].

References:

[1]. ARYL SULFONOHYDRAZIDES. WO2016198507 A1.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
2055397-18-5
同义词
WM8014,WM 8014
化学名
N'-(4-fluoro-5-methyl-[1,1'-biphenyl]-3-carbonyl)benzenesulfonohydrazide
SMILES
O=S(C1=CC=CC=C1)(NNC(C2=C(F)C(C)=CC(C3=CC=CC=C3)=C2)=O)=O
分子式
C20H17FN2O3S
分子量
384.42 g/mol
溶解性
DMF: 50 mg/ml,DMF:PBS (pH 7.2) (1:7): 0.1 mg/ml,DMSO: 33 mg/ml,Ethanol: 2 mg/ml
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol