bobcat339

Description: Bobcat339 is a novel and potent cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2). Bobcat339 has mid-uM inhibitor activity against TET1 and TET2, but does not inhibit the DNA methyltransferase, DNMT3a. In silico modeling of the TET enzyme active site is used to rationalize the activity of Bobcat339 and other cytosine-based inhibitors. These new molecular tools will be useful to the field of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription. It is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.

References: ACS Med Chem Lett. 2019 Jan 31; 10(2):180-185.