SML2174
MS012
≥98% (HPLC)
Synonym(s):
N2-Hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine
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About This Item
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assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
CN(CC1)CCC1NC2=C3C(C=C(OC)C(OC)=C3)=NC(NCCCCCC)=N2
Biochem/physiol Actions
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_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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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.
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
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