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A-366 {[allProObj[0].p_purity_real_show]}

货号:A120345 Ambeed 开学季,买赠积分,赢豪礼

A-366 is a peptide-competitive inhibitor of G9a/GLP with IC50 of ~3 nM.

A-366 化学结构 CAS号:1527503-11-2
A-366 化学结构
CAS号:1527503-11-2
A-366 3D分子结构
CAS号:1527503-11-2
A-366 化学结构 CAS号:1527503-11-2
A-366 3D分子结构 CAS号:1527503-11-2
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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: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 {[allProObj[0].p_purity_real_show]}
UNC1999 +++

EZH2, IC50: 2 nM

EZH1, IC50: 45 nM

{[allProObj[0].p_purity_real_show]}
EPZ005687 ++

EZH2, Ki: 24 nM

{[allProObj[0].p_purity_real_show]}
EPZ015666 +++

PRMT5, Ki: 5 nM

{[allProObj[0].p_purity_real_show]}
3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

{[allProObj[0].p_purity_real_show]}
EPZ6438 +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

{[allProObj[0].p_purity_real_show]}
GSK126 ++

EZH2, IC50: 9.9 nM

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MI-3 +

Menin-MLL, IC50: 648 nM

{[allProObj[0].p_purity_real_show]}
MM-102 ++

MLL1, IC50: 0.4 μM

{[allProObj[0].p_purity_real_show]}
EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

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SGC0946 ++++

DOT1L, IC50: 0.3 nM

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PFI-2 HCl ++++

SETD7, IC50: 2 nM

SETD7, Ki: 0.33 nM

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Pinometostat ++++

DOT1L, Ki: 80 pM

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EPZ004777 +++

DOT1L, IC50: 0.4 nM

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Entacapone ++

COMT, IC50: 151 nM

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UNC0379 +

SETD8, IC50: 7.9 μM

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Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

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GSK343 +++

EZH2, IC50: 4 nM

EZH1, IC50: 240 nM

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BIX-01294 3HCl +

G9a, IC50: 2.7 μM

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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]. 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]

A-366 动物研究

Dose Mice: 1 mg/kg, 2 mg/kg[4] (i.p.); 30 mg/kg[5] (osmotic mini-pump, OMP)
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.

A-366 实验方案

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

CAS号1527503-11-2
分子式C19H27N3O2
分子量 329.437
别名
运输蓝冰
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
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