A-366 | G9a/GLP inhibitor | Probechem Biochemicals

Chemical Structure : A-366

CAS No.: 1527503-11-2

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A-366 (A366)

货号: PC-43110Not For Human Use, Lab Use Only.

A-366 is a potent, highly selective inhibitor of histone methyltransferase G9a/GLP with IC50 of 3/38 nM, >1,000-fold selectivity for G9a over 21 other methyltransferases.

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10 mg	￥880	In stock
25 mg	￥1380	In stock
50 mg	￥2180	In stock
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生物&药学活性

A-366 is a potent, highly selective inhibitor of histone methyltransferase G9a/GLP with IC50 of 3/38 nM, >1,000-fold selectivity for G9a over 21 other methyltransferases.
A-366 effects a clear reduction in H3K9 methylation in cells, shows significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2 (H3K9me2 cellular EC50=0.3 uM).
A-366 induces differentiation and affects viability in MV4;11 cells, demonstrates growth inhibition in vivo consistent with the profile of H3K9me2 reduction in flank xenograft leukemia model.

物理化学性质&存储条件

分子量	329.4366
分子式	C19H27N3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-

参考文献

1. Sweis RF, et al. ACS Med Chem Lett. 2014 Jan 2;5(2):205-9.

2. Pappano WN, et al. PLoS One. 2015 Jul 6;10(7):e0131716.

3. Agarwal P, et al. Cancer Lett. 2016 Oct 1;380(2):467-75.

A-366 (A366)

生物&药学活性

物理化学性质&存储条件

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A-366 (A366)

生物&药学活性

物理化学性质&存储条件

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