Tag: H3K4

E67-2 is a Selective KIAA1718 Jumonji Domain Inhibitor with Low Toxicity

KIAA1718 is a histone demethylase for repressive methyl marks. what’s more, KIAA1718 involves in transcriptional activation. Specifically, KIAA1718, as a PHF2/PHF8 subfamily member, possesses histone demethylase activity specific for histone H3 lysine 9 (H3K9) and histone H3 lysine 9 (H3K27), transcriptionally repressive histone marks. Furthermore, KIAA1718 forms complexes with...

MRK-740 is a Selective and PRDM9 Histone Methyltransferase Inhibitor

PRDM9 is a zinc finger protein that binds DNA at specific locations in the genome and alleles influence human chromosomal rearrangements, causing hereditary diseases. MRK-740 is a potent selective and cell-active PRDM9 inhibitor with an IC50 of 80 nM. In cells, MRK-740 specifically and directly inhibits H3K4 methylation at endogenous...