UNC0638 - 10mM in DMSO, high purity , CAS No.1255580-76-7

Item Number

U421071

• Synonyms: 1255580-76-7 | UNC0638 | UNC-0638 | UNC 0638 | 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine | 1255517-77-1 | 2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: UNC0638 is selective for G9a (EHMT2) and GLP (EHMT1) methyltransferases, which can catalyze the methylation of lysine 9 of histone 3 (H3K9) and other non-histone substrates.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Description
UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities.
Application
In MDA-MB-231 cells, in a concentration-dependent manner, exposure to UNC0638 for 48 h reduced H3K9me2 levels with an IC50 value of 81 ± 9 nM. Cellular levels of H3K9me2 were progressively reduced from 1 d to 4 d exposure to UNC0638 at the concentrations of 80 nM (IC50), 250 nM (IC90) and 500 nM (2 × IC90). The reductions of H3K9me2 levels with 250 nM and 500 nM treatments after 4 d were equal or very close to that of G9a and GLP knockdown cells. The effects of UNC0638 were long-lasting. In cells with 2 d exposure to UNC0638, levels of H3K9me2 remained low after washout of compound followed by 2 d incubation without the inhibitor.