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A chemical tool for in vitro and in vivo precipitation of lysine methyltransferase G9a.

ABSTRACT: Here we report the design, synthesis, and biochemical characterization of a new chemical tool, UNC0965. UNC0965 is a biotinylated version of our previously reported G9a chemical probe, UNC0638. Importantly, UNC0965 maintains high in vitro potency and is cell penetrant. The biotinylated tag of UNC0965 enables "chemiprecipitation" of G9a from whole cell lysates. Further, the cell penetrance of UNC0965 allowed us to explore the localization of G9a on chromatin both in vitro and in vivo through chemical inhibitor-based chromatin immunoprecipitation (chem-ChIP).

SUBMITTER: Konze KD

PROVIDER: S-EPMC4005005 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature

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A chemical tool for in vitro and in vivo precipitation of lysine methyltransferase G9a.

Konze Kyle D KD Pattenden Samantha G SG Liu Feng F Barsyte-Lovejoy Dalia D Li Fengling F Simon Jeremy M JM Davis Ian J IJ Vedadi Masoud M Jin Jian J

ChemMedChem 20140117 3

Here we report the design, synthesis, and biochemical characterization of a new chemical tool, UNC0965. UNC0965 is a biotinylated version of our previously reported G9a chemical probe, UNC0638. Importantly, UNC0965 maintains high in vitro potency and is cell penetrant. The biotinylated tag of UNC0965 enables "chemiprecipitation" of G9a from whole cell lysates. Further, the cell penetrance of UNC0965 allowed us to explore the localization of G9a on chromatin both in vitro and in vivo through chem ...[more]

PMID: 24443078

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Protein lysine methyltransferase G9a acts on non-histone targets.

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Lysine methyltransferase G9a is an important modulator of trained immunity.

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