Methyllysine (Kme) recognition “reader” domains play a central role in epigenetic regulation during cellular differentiation, development, and gene transcription. UNC1215 is a potent and selective chemical probe for the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors. UNC1215 binds L3MBTL3 with a Kd value of 120 nM (IC50 = 40 nM), competitively displacing mono- or dimethyl-lysine containing peptides. This probe is greater than 50-fold selective toward L3MBTL3 than other members of the human MBT family and demonstrates selectivity against more than 200 other Kme reader domains examined. See the Structural Genomics Consortium (SGC) website for more information.
