Potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5nM). Exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. Reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110nM). Displays modest brain penetration in vivo.
Chemical Name: 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
CAS Number: 1481677-78-4
Solubility: Soluble to 100mM in DMSO and to 50mM in 1eq. HCl
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