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420205 Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem

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420205-10MG
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      Glasflasche 10 mg
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      Description
      OverviewA cell-permeable GSK-J1 (Cat. No. 420204) prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50 µM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-α production in primary human macrophage cultures (IC50 = 9 µM by ELISA).

      This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the SGC website (http://www.thesgc.org/scientists/chemical_probes/GSKJ1).
      Catalogue Number420205
      Brand Family Calbiochem®
      SynonymsGSK-J1 Pro-Drug, JHDM Inhibitor II Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate
      References
      ReferencesHeinemann, B., et al. 2014. Nature 514 E1.
      Kruidenier, L., et al. 2014. Nature 514, E2.
      Kruidenier, L., et al. 2012. Nature 488, 404.
      Product Information
      CAS number1373423-53-0
      FormTan semi-solid
      Hill FormulaC₂₄H₂₇N₅O₂
      Chemical formulaC₂₄H₂₇N₅O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationHistone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 µM in HeLa cultures).
      Biological Information
      Primary TargetH3K27me3 demethylases JMJD3 & UTX
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      420205-10MG 04055977210798