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检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
CN(CC1)CCC1NC2=C3C(C=C(OC)C(OC)=C3)=NC(NCCCCCC)=N2
生化/生理作用
MS012 is a selective G9a-like Protein (GLP) lysine methyl transferase (PKMT) inhibitor with an IC50 value of 7 nM and over 140-fold selectivity for GLP over G9a and other methyl transferases tested.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Journal of medicinal chemistry, 60(5), 1876-1891 (2017-01-31)
G9a-like protein (GLP) and G9a are highly homologous protein lysine methyltransferases (PKMTs) sharing approximately 80% sequence identity in their catalytic domains. GLP and G9a form a heterodimer complex and catalyze mono- and dimethylation of histone H3 lysine 9 and nonhistone
Bioorganic & medicinal chemistry, 25(16), 4414-4423 (2017-07-01)
Given the high homology between the protein lysine methyltransferases G9a-like protein (GLP) and G9a, it has been challenging to develop potent and selective inhibitors for either enzyme. Recently, we reported two quinazoline compounds, MS0124 and MS012, as GLP selective inhibitors.
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