Inside Cover: A Chemical Tool for In Vitro and In Vivo Precipitation of Lysine Methyltransferase G9a (ChemMedChem 3/2014)
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 UNC096...
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| Veröffentlicht in: | ChemMedChem 2014-03, Vol.9 (3), p.414-414 |
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| creator | Konze, Kyle D. Pattenden, Samantha G. Liu, Feng Barsyte-Lovejoy, Dalia Li, Fengling Simon, Jeremy M. Davis, Ian J. Vedadi, Masoud Jin, Jian |
| description | 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). |
| doi_str_mv | 10.1002/cmdc.201490006 |
| format | Article |
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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).</description><identifier>ISSN: 1860-7179</identifier><identifier>EISSN: 1860-7187</identifier><identifier>DOI: 10.1002/cmdc.201490006</identifier><language>eng</language><publisher>Weinheim: WILEY-VCH Verlag</publisher><subject>chromatin ; enzymes ; G9a ; lysine methyltransferase ; medicinal chemistry</subject><ispartof>ChemMedChem, 2014-03, Vol.9 (3), p.414-414</ispartof><rights>2014 WILEY-VCH Verlag GmbH & Co. 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| fulltext | fulltext |
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| ispartof | ChemMedChem, 2014-03, Vol.9 (3), p.414-414 |
| issn | 1860-7179 1860-7187 |
| language | eng |
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| source | Wiley Online Library Journals Frontfile Complete |
| subjects | chromatin enzymes G9a lysine methyltransferase medicinal chemistry |
| title | Inside Cover: A Chemical Tool for In Vitro and In Vivo Precipitation of Lysine Methyltransferase G9a (ChemMedChem 3/2014) |
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