WM-8014
产品说明书
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同义名 : | MOZ-IN-3 |
| CAS号 : | 2055397-18-5 | |
| 货号 : | A613796 | |
| 分子式 : | C20H17FN2O3S | |
| 纯度 : | 99%+ | |
| 分子量 : | 384.42 | |
| MDL号 : | MFCD31630714 | |
| 存储条件： |
Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MYST proteins are the largest family of Histone acetyltransferases (HATs) and have a conserved MYST domain responsible for the acetyl transferase activity[1]. MOZ-IN-3, also known as WM8013, is a selective inhibitor of KAT6A, KAT6B, KAT5 and KAT7 of MYST with IC50 values of 8nM, 28nM, 224nM and 342nM, respectively. In vitro, MOZ-IN-3 inhibited MEFs proliferate after 10 days of treatment with IC50 value of 2.4nM. Treatment with 10μM MOZ-IN-3 for 6 days increased the proportion of cells in G0/G1 and a corresponding reduction in cells in G2/M and S phases. In addition, MOZ-IN-3 increased the β-galactosidase activity and Cdkn2a mRNA expression. These results showed that MOZ-IN-3 causing cell cycle arrest leading to senescence. Treatment with 10μM MOZ-IN-3 directly inhibited global H3K14 acetylation catalyzed by KAT7, and KAT6A-specific H3K9 acetylation at transcription start sites. MOZ-IN-3 also inhibited the proliferation of B cell lymphoma cell line EMRK1184 with IC50 value of 2.3μM. Treatment with 10μM MOZ-IN-3 potentiated oncogene-induced senescence without affect the growth of the normal hepatocyte in the zebrafish model hepatocellular carcinoma. However, the plasma protein binding of MOZ-IN-3 more was greater than 99.9% precluding in vivo studies in mice[2]. | ||
| 作用机制 | MOZ-IN-3 competes directly with acetyl-CoA in the MYST lysine acetyltransferase domain[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.60mL 0.52mL 0.26mL |
13.01mL 2.60mL 1.30mL |
26.01mL 5.20mL 2.60mL |
| 参考文献 |
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