KMT9-IN-1

KMT9-IN-1 (also known as KMT9 inhibitor prodrug 8 or Compound 8) is the ethyl ester prodrug form of a potent and selective lysine methyltransferase 9 (KMT9) inhibitor, specifically KMT9 inhibitor 7b. KMT9-IN-1 is designed to increase cell permeability and releases its active parent compound (7b) intracellularly via esterase-mediated hydrolysis. Its mechanism of action is selective inhibition of KMT9, a histone lysine methyltransferase that monomethylates histone H4 at lysine 12 (H4K12me1). This results in reduced levels of H4K12me1 and inhibition of genes involved in cell cycle regulation, ultimately leading to suppression of proliferation in tumor cell lines, particularly colon cancer. KMT9-IN-1 exhibits cellular target engagement and efficacy in reducing cancer cell proliferation, making it a promising preclinical tool for epigenetic cancer therapy research[1][2][4][5][6].

Other names

KMT9 inhibitor 8KMT-9 inhibitor 8KMT 9 inhibitor 8Compound 8Compound8Compound-8