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CAS No.: 2055397-28-7

WM-1119 Catalog No. CSN22467

Synonyms: MOZ-IN-1

MOZ-IN-1 is an inhibitor of MOZ which is a member of histone acetyltransferases with IC50 of 0.051 μM.

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实验方案

技术信息

生物活性

描述Histone acetyltransferases (HATs) play a vital role in a range of epigenetic pathways by the acetylation of histones using acetyl-CoA as substrate. MYST family is responsible for a wide range of cellular events and comprising approximately one-third in the human genome. WM-119 is a selective inhibitor of KAT6A of MYST^[1]. WM119 can bind to KAT6A, KAT5 and KAT7 at a binding KD values of 2 nM, 2.2 μM and 0.5 μM, respectively. In vitro, treatment with WM-1119 resulted in increased levels of Cdkn2a and Cdkn2b mRNA and P16 and P19 proteins, as well as a delayed increase in Cdkn1a mRNA. WM-1119 inhibited the proliferation of B cell lymphoma cell line EMRK1184 with IC50 value of 0.25 μM. Treatment of mouse embryonic fibroblasts (MEFs) with 1 μM WM-1119 induced cell cycle arrest in G1 and a senescence phenotype. In vivo, administered WM-1119 at 50 mg/kg via intraperitoneal injection four times daily for 14 days substantially reduced the level of H3K9ac in lymphoma cells, and the proportion and overall number of lymphoma cells in mice, suggesting that WM-1119 was effective in treating lymphoma in vivo^[2].
作用机制M-1119 competes with acetyl-CoA in the MYST lysine acetyltransferase domain^[2].
参考文献

[1] Priebbenow DL, Leaver DJ, Nguyen N, Cleary B, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Shackleford DM, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Jousset Sabroux H, Falk H, Chung MC, Hermans SJ, Downer NL, Parker MW, Voss AK, Thomas T, Baell JB. Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents. J Med Chem. 2020 May 14;63(9):4655-4684.
[2] Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257.

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
- 2.5682 mL
- 12.8409 mL
- 25.6819 mL
- 5 mM
- 0.5136 mL
- 2.5682 mL
- 5.1364 mL
- 10 mM
- 0.2568 mL
- 1.2841 mL
- 2.5682 mL

技术信息

CAS号

2055397-28-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H13F2N3O3S

运输

蓝冰

分子量

389.38

别名

MOZ-IN-1

溶解度

DMSO	410.0 mg/mL (1053.0 mM)
Water	insoluble

动物实验配方

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WM-1119 Catalog No. CSN22467

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