UNC0642 : Peptide substrate competitive, SAM noncompetitive inhibitor of EHMT2 and EHMT1
- Peptide substrate competitive inhibitor, SAM noncompetitive inhibitor
In Vitro Validations
DOI Reference: 10.1021/jm401480r
In Cell Validations
In Vivo Data
Off-Target Selectivity Assesments
UNC0642 was 2,000-fold selective for the targets over EZH2/PRC2 and 20,000-fold over 15 other protein methyltransferases. No activity was detected against 50 kinases. <50% inhibitory activity was detected against a panel of 44 GPCRs, ion channels, and transporters at 1 uM, except histamine H3 receptor (Ki = 45 nM).