A cell-permeable analog of the amino-benzimidazolo BIX-01338 and the methylester prodrug of BRD9539 that acts as an SAM-competitive inhibitor against PRC2 and G9a (IC50<6.3uM) histone methyltransferase activities, displaying little effect toward 10 other HMTases, 9 HDACs, and 100 cellular kinases. Selectively reduces H3K9me2 and H3K9me3 (EC50=5uM) histone methylation levels in pancreatic cancer cells (PANC-1) with much less or little effect toward H3K36me3, H3K4me3, H3K27me3, or H3K6me3 levels. Inhibits both anchorage-dependent and -independent PANC-1 proliferation via ATM activation and G2/M cell-cycle arrest, but not apoptosis induction (no caspase3/7 activation; 10uM, 72h).
Formula:C25H23N3O3
Primary Target:G9a and PRC2 HMTases
Solubility:DMSO
Molecular Weight:413.5
Storage and Stability:Store at 4°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.