MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively.

METHODS: Human cervical cancer HeLa cells were treated with MAK683 (1.5-370nM) for 72 hours, and H3K27me3 protein expression was observed by Western Blot experiment.
RESULTS MAK683 dose-dependently inhibited H3K27me3 protein expression in HeLa, with an IC50 of approximately 1.014nM. [1]

METHODS: To detect anti-tumor activity in vivo, WT G401 or p16 knockout cells were washed and resuspended in cold PBS. The tumor cell mixture was then injected subcutaneously into female Balb/c nude mice. When the tumor volume reached about 60-350 mm, The mice were numbered and randomly assigned to the 100 mg/kg MAK683 treatment group, which was administered at 8 a.m. The mouse body weight and tumor volume were measured and recorded every 3 days. RESULTS MAK683 treatment significantly inhibited the proliferation of female mouse G401 WT or p16 KO cells. [1]