WM-8014

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WM-8014  纯度: 99.64%

WM-8014 是一种 MOZ (属于 histone acetyltransferases) 的抑制剂,IC50 值为 55 nM。

WM-8014

WM-8014 Chemical Structure

CAS No. : 2055397-18-5

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥4800 In-stock
25 mg ¥9600 In-stock
50 mg ¥15000 In-stock
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WM-8014 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.

IC50 & Target

IC50: 55 nM (MOZ)[1]

体外研究
(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%[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

384.42

Formula

C20H17FN2O3S

CAS 号

2055397-18-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 250 mg/mL (650.33 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6013 mL 13.0066 mL 26.0132 mL
5 mM 0.5203 mL 2.6013 mL 5.2026 mL
10 mM 0.2601 mL 1.3007 mL 2.6013 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.50 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. ARYL SULFONOHYDRAZIDES. WO2016198507 A1.

Kinase Assay
[1]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. ARYL SULFONOHYDRAZIDES. WO2016198507 A1.

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