UNC0638

UNC0638 is a potent, selective, cell-penetrant small-molecule inhibitor of the histone lysine methyltransferases G9a (EHMT2) and GLP (EHMT1)[1][2][4][7]. It inhibits the dimethylation of histone H3 on lysine 9 (H3K9me2), a modification associated with transcriptional repression, with high potency (IC50 < 15 nM for G9a, < 20 nM for GLP)[2]. UNC0638 demonstrates low toxicity and high selectivity, showing minimal off-target effects at recommended concentrations, and is widely used as an epigenetic chemical probe for studying G9a/GLP biology in vitro and in vivo[1][4][7]. Biologically, UNC0638 has been shown to suppress epithelial-mesenchymal transition and reduce invasion/metastasis in various cancer models such as triple-negative breast cancer and neuroblastoma, among other indications[3][6]. It may also increase fetal hemoglobin expression in erythroid cells[9].

Other names

CS-565CS565CS 565HMTase Inhibitor IV, UNC06382-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine2-Cyclohexyl-N-(1-isopropyl-4-piperidinyl)-6-Methoxy-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinaMine2-cyclohexyl-6-methoxy-n-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine2-Cyclohexyl-6-Methoxy-N-[1-(1-Methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinaMine1255580-76-7CHEMBL1231795CHEMBL-1231795CHEMBL 1231795CHEBI:95074UNII:26A103L2FO