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CAS No.: 2055397-18-5

WM-8014 Catalog No. CSN21259

Synonyms: MOZ-IN-3;Compound 36

MOZ-IN-3 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.

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技术信息

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].
参考文献

[1] Leaver DJ. Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A. J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665. Epub 2019 Jul 17.
[2] Baell JB. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6013 mL
- 13.0065 mL
- 26.0129 mL
- 5 mM
- 0.5203 mL
- 2.6013 mL
- 5.2026 mL
- 10 mM
- 0.2601 mL
- 1.3006 mL
- 2.6013 mL

技术信息

CAS号

2055397-18-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H17FN2O3S

运输

蓝冰

分子量

384.42

别名

MOZ-IN-3;Compound 36

溶解度

DMSO	77.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	Insoluble

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WM-8014 Catalog No. CSN21259

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