MS453 is a potent and selective inhibitor of the histone methyltransferase SETD8, exhibiting an IC50 of 804 nM. It preferentially targets a cysteine residue adjacent to the binding site, demonstrating specificity over 28 other methyltransferases. The crystal structure elucidates the binding mode of MS453 to SETD8, offering valuable insights for the design of advanced chemical probes aimed at this important target in epigenetic regulation.
MS453 is a potent and selective inhibitor of the histone methyltransferase SETD8, exhibiting an IC50 of 804 nM. It preferentially targets a cysteine residue adjacent to the binding site, demonstrating specificity over 28 other methyltransferases. The crystal structure elucidates the binding mode of MS453 to SETD8, offering valuable insights for the design of advanced chemical probes aimed at this important target in epigenetic regulation.
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