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A-366

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Chemical Structure| 1527503-11-2 同义名 : -
CAS号 : 1527503-11-2
货号 : A120345
分子式 : C19H27N3O2
纯度 : 98%
分子量 : 329.437
MDL号 : MFCD28133403
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(151.77 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 A-366 is a potent G9a inhibitor with IC50 value of 3.3nM. It inhibited cellular H3K9Me2 in a dose-dependent manner at concentration<10μM in PC3 cells after 72-hour treatment[4]. Administration of A-366 at dose of 4mg/kg, i.p., reduced anxiety-like behaviors of adult mice, in conjunction with decreased H3K9 methylation in the brain[5]. A-366 hypersensitised tumour cells to low doses of DSB-inducing agents[6].
作用机制 A-366 binds to the substrate peptide site on G9a, competitive with the substrate and non-competitive with the cofactor SAM.[4]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.04mL

0.61mL

0.30mL

15.18mL

3.04mL

1.52mL

30.35mL

6.07mL

3.04mL
参考文献

[1]Sweis RF, Pliushchev M, et al. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014 Jan 2;5(2):205-9.

[2]Wang X, Wang H, et al. Genetic variation in ZmVPP1 contributes to drought tolerance in maize seedlings. Nat Genet. 2016 Oct;48(10):1233-41.

[3]Agarwal P, Jackson SP, et al. G9a inhibition potentiates the anti-tumour activity of DNA double-strand break inducing agents by impairing DNA repair independent of p53 status. Cancer Lett. 2016 Oct 1;380(2):467-75.

[4]Sweis RF, Pliushchev M, Brown PJ, Guo J, Li F, Maag D, Petros AM, Soni NB, Tse C, Vedadi M, Michaelides MR, Chiang GG, Pappano WN. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014 Jan 2;5(2):205-9. doi: 10.1021/ml400496h. PMID: 24900801; PMCID: PMC4027767.

[5]Wang X, Wang H, Liu S, Ferjani A, Li J, Yan J, Yang X, Qin F. Genetic variation in ZmVPP1 contributes to drought tolerance in maize seedlings. Nat Genet. 2016 Oct;48(10):1233-41. doi: 10.1038/ng.3636. Epub 2016 Aug 15. PMID: 27526320.

[6]Agarwal P, Jackson SP. G9a inhibition potentiates the anti-tumour activity of DNA double-strand break inducing agents by impairing DNA repair independent of p53 status. Cancer Lett. 2016 Oct 1;380(2):467-475. doi: 10.1016/j.canlet.2016.07.009. Epub 2016 Jul 16. PMID: 27431310; PMCID: PMC5011428.