A cytosine derivative
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Bobcat 339 is an inhibitor of ten-eleven translocation methylcytosine dioxygenase 1 (TET1) and TET2 (IC50s = 33 and 73 µM, respectively).1 It is selective for TET1 and TET2 over DNA methyltransferase 3a (DNMT3a) at 500 µM. Bobcat 339 (10 µM) reduces DNA 5-hydroxymethylcytosine (5-hmC) levels in HT22 hippocampal neurons.
1.Chua, G.N.L., Wassarman, K.L., Sun, H., et al.Cytosine-based TET enzyme inhibitorsACS Med. Chem. Lett.10(2)180-185(2019)