Extended Data Fig. 4: Design and synthesis of H3K36-JmjC inhibitor covalent conjugate.
From: Structural basis of paralog-specific KDM2A/B nucleosome recognition
a, Chemical structures of JmjC inhibitors. b, Inhibition assays using H3K36me2 peptide substrates with KDM2B(2–734). c, Dose response inhibition of KDM2B(2–734) by UNC8016 on H3K36me2 peptide substrates. In b and c, mean ± SD are shown (n = 3 assay technical replicates). d, Synthetic scheme for alkylation reaction of H3K36C mutant with UNC8015. e, LCMS spectra and mass deconvolution (determined using ESIprot) of unreacted H3K36C (left) and reacted H3K36C-UNC8015 (right; 5-hour endpoint).
