WM-1119

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Chemical Structure| 2055397-28-7 同义名 : -
CAS号 : 2055397-28-7
货号 : A573581
分子式 : C18H13F2N3O3S
纯度 : 99%+
分子量 : 389.376
MDL号 : MFCD31690337
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(308.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.84mL

2.57mL

1.28mL

25.68mL

5.14mL

2.57mL
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.