A-366
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货号：A120345
A-366 is a peptide-competitive inhibitor of G9a/GLP with IC50 of ~3 nM.
A-366 化学结构
A-366 3D分子结构
规格
价格
会员价
库存
数量
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A-366 纯度/质量文件 产品仅供科研
货号：A120345
标准纯度：
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产品说明书
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A-366 质控信息
BRD4770
✔
99%+
UNC1999
+++
EZH2, IC50: 2 nM
EZH1, IC50: 45 nM
99%+
EPZ005687
++
98+%
EPZ015666
+++
99%+
3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
99%+
Tazemetostat
+++
EZH2, IC50: 11 nM
EZH2, Ki: 2.5 nM
98%
GSK126
++
99%+
MI-3
+
98%
MM-102
++
99%
EI1
++
EZH2 (Y641F), IC50: 13 nM
Ezh2 (wild-type), IC50: 15 nM
98%
SGC0946
++++
99%+
PFI-2 HCl
++++
SETD7, Ki: 0.33 nM
SETD7, IC50: 2 nM
99%+
Pinometostat
++++
99%+
EPZ004777
+++
99%+
Entacapone
++
95%
UNC0379
+
99%+
Menin-MLL inhibitor MI-2
+
98%
GSK343
+++
EZH2, IC50: 4 nM
EZH1, IC50: 240 nM
99%+
BIX-01294 3HCl
+
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
A-366 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] [5] [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]
A-366 动物研究
Dose
Mice: 1 mg/kg, 2 mg/kg[4] [5]
Administration
i.p., OMP
A-366 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.
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A-366 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
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
A-366 技术信息
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