UNC1999
Methyltransferase inhibitor / UNC1999 is an orally bioavailable, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50’s = 45 nM and 2 nM respectively).1 Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells
Biochemicals & reagents
1431612-23-5
1) Konze et al. (2013), An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1; ACS Chem.Biol. 8 1324 2) Katona et al. (2014), EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells; Cancer Biol.Ther., 15 1677
-20°C
TARGET: Protein methyltransferase -- PATHWAY: Chromatin; Posttranslational modification; Proliferation -- RESEARCH AREA: Epigenetics; Stem cells -- DISEASE AREA: Cancer