Uses
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription[1].
Biological Activity
Bobcat339 is a cell penetrant, potent and selective inhibitor of TET1 and TET2 [Ten-eleven translocation methylcytosine dioxygenase (TET) 1 and 2] th at reduces content of 5-hydroxymethyl-cytosine (5hmC) in cultured neurons. Bobcat339 does not inhibit DNMT3a.
IC 50
TET1: 33 μM (IC
50); TET2: 73 μM (IC
50)
References
[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
