2436747-44-1

Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription[1].

TET1: 33 μM (IC₅₀); TET2: 73 μM (IC₅₀)

[1] Chua GNL, et al. Cytosine-Based TET Enzyme Inhibitors. ACS Med Chem Lett. 2019 Jan 31;10(2):180-185. DOI:10.1021/acsmedchemlett.8b00474
[2] Weirath NA, et al. Small Molecule Inhibitors of TET Dioxygenases: Bobcat339 Activity Is Mediated by Contaminating Copper(II). ACS Med Chem Lett. 2022 Apr 21;13(5):792-798. DOI:10.1021/acsmedchemlett.1c00677