A-366
Cat. No.:YN310180
产品名称: | A-366 |
CAS No.: | 1527503-11-2 |
Chemical Name: | 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-spiro[cyclobutane-1,3'-[3H]indol]-2'-amine |
Synonyms: | A 366,A366 |
分子量: | 329.44 |
分子式: | C₁₉H₂₇N₃O₂ |
SMILES: | COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | A-366 是一种高效、高选择性的肽竞争性组蛋白甲基转移酶G9a抑制剂,对 G9a 和 GLP 的IC50分别为 3.3 和 38 nM。A-366 比其他 21 种甲基转移酶具有 1000 倍以上的选择性。A-366 是一种有效的Spindlin1-H3K4me3相互作用的抑制剂 (IC50=182.6 nM)。A-366 对人 H3R (Ki=17 nM) 表现出很高的亲和力,并且在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。 |
IC50和靶点: | |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Sweis, R.F., Pliushchev, M., Brown, P.J., et al.Discovery and development of potent and selective inhibitors of histone methyltransferase G9aACS Med. Chem. Lett.5(2),205-209(2014)
Wagner, T., Greschik, H., Burgahn, T., et al.Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platformNucleic Acids Res.,(2016)