GSK343 is a potent, selective inhibitor of EZH2 with cellular activity. GSK343 inhibits EZH2 with an IC50 of 4nM and is over 1000-fold selective for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC50 of <200nM as measured by immunofluorescence. GSK343 exhibited limited effects on the growth of EOC cells in conventional two-dimensional (2D) culture. In contrast, GSK343 significantly suppressed the growth of EOC cells cultured in 3D matrigel extracellular matrix (ECM), which more closely mimics the tumor microenvironment in vivo. Notably, GSK343 induces apoptosis of EOC cells in 3D but not 2D culture. In addition, GSK343 significantly inhibited the invasion of EOC cells.
Histone Methyltransferase Inhibitors Related Products:
EPZ005687; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; HLCL-61 HCL; GSK591; SGC707; GSK503; EPZ015666; PFI-2 HCl; UNC0642; UNC0638; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770; Pinometostat