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Description

"A nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of ""chromatin lock"" L3MBTL1 (Lethal 3 MBT-Like protein 1, Kd = 5 µ,M by Isothermal titration calorimetry) that ""reads""/binds mono- and dimethyl-lysine modified histones as well as other proteins involved in transcription, such as p53 and Rb, via methylation-dependent recognition. Shown to effectively compete against FAM-labeled, monomethylated Histone H3 (1-15) peptide (H3K9Me1) binding to L3MBTL1 (Kd = 10 µ,M in a FP displacement assay) and exhibit higher affinity toward L3MBTL1 than L3MBTL3 and L3MBTL4 (IC50 = 6, 35, and 69 µ,M, respectively, in a luminescent peptide competitive binding assay), while displaying no detectable binding toward four other methyl-lysine-binding proteins, the BMT domain-containing SFMBT1 and MBTD1, the PHD (Plant Homeodomain) finger-containing PHF13 (PHD finger 13), and the chromo domain-containing CBX7 (chromobox 7). As of end of 2012, no published data is available regarding the molecule's permeability or biological activity in cells."