Catalog No.: PC-20645Not For Human Use, Lab Use Only.
HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9a/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2).
HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9a/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2).
HKMTI-1-005 inhibits MDA-MB-231 cell growth with IC50 of 4.3 uM in MTT assays, induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, as measured by Caspase 3/7 activity.
HKMTI-1-005 induces chromatin changes that resulted in the transcriptional activation of immunostimulatory gene networks, including the re-expression of elements of the ERV-K endogenous retroviral family.
HKMTI-1-005 improved the survival of mice bearing Trp53-/- null ID8 ovarian tumors and resulted in tumor burden reduction.
HKMTI-1-005 phenocopied EZH2 knockdown and was more effective in inducing differentiation than GSK-343.
