WM-8014
(Synonyms: WM8014,WM 8014) 目录号 : GC18153
An inhibitor of KAT6A and KAT6B
Cas No.:2055397-18-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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).
(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.)
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.
| Cas No. | 2055397-18-5 | SDF | |
| 别名 | WM8014,WM 8014 | ||
| 化学名 | N'-(4-fluoro-5-methyl-[1,1'-biphenyl]-3-carbonyl)benzenesulfonohydrazide | ||
| Canonical 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 |
| 溶解度 | DMF: 50 mg/ml,DMF:PBS (pH 7.2) (1:7): 0.1 mg/ml,DMSO: 33 mg/ml,Ethanol: 2 mg/ml | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。