UNC1999

UNC1999 (1431612-23-5) 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 (Cat.# 10-1148) in suppressing the proliferation of colon cancer cells References/Citations: 1) Konze et al. (2013), An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1; ACS Chem. Biol., 8 13242) Katona et al. (2014), EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells; Cancer Biol. Ther., 15 1677 CAS: 1431612-23-5 Catalog Number: 10-4542 Activity: Methyltransferase inhibitor Chemical Name: N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide Molecular Weight: 569.74 Molecular Formula: C33H43N7O2 Solubility: Soluble in DMSO (up to 10 mg/ml). Physical Pro