Bobcat339

Bobcat339 is a small-molecule inhibitor and degrader of the Ten-Eleven Translocation (TET) family of enzymes, specifically TET1, TET2, and TET3. These enzymes are methylcytosine dioxygenases that catalyze the conversion of 5-methylcytosine (5mC) to 5-hydroxymethylcytosine (5hmC), a critical step in active DNA demethylation. Bobcat339 is a synthetic cytosine derivative that has demonstrated therapeutic potential in various preclinical models, including cancer (bladder, hepatocellular, and breast), cardiovascular diseases (myocardial fibrosis and vascular calcification), and psychiatric or neurological conditions (PTSD, anorexia nervosa, and chronic pain). Mechanistically, it has been shown to induce the degradation of TET3 via a von Hippel-Lindau (VHL) E3 ubiquitin ligase-dependent pathway. Additionally, Bobcat339 has been identified as a non-nucleoside inhibitor of the SARS-CoV-2 nonstructural protein 14 (nsp14) N7-methyltransferase, which is essential for viral RNA capping and replication. However, its biochemical potency as a TET inhibitor has been a subject of debate, with some studies suggesting that its activity may be mediated or enhanced by copper(II) contamination.

Other names

Bobcat339 hydrochlorideBobcat-339 hydrochlorideBobcat 339 hydrochloride