Methylst at is an inhibitor of the Jumonji C domain-containing histone trimethyl demethylases (JHDMs). Methylst at inhibits the activity of JMJD2C (IC50 = 4.3 μM), with similar potency against JMJD2E and JMJD3. The compound has poor activity against dimethyl demethylases, and does not inhibit class I or II HDACs. Methyls at blocks proliferation of the esophageal carcinoma cell line KYSE150 with an IC50 value of 5.1 μM.
