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

Histone 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).

Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: GSK-J1 Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug

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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, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug
      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
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      420205-10MG 04055977210798

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      420205

      References

      Reference overview
      Heinemann, B., et al. 2014. Nature 514 E1.
      Kruidenier, L., et al. 2014. Nature 514, E2.
      Kruidenier, L., et al. 2012. Nature 488, 404.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision06-September-2013 JSW
      SynonymsGSK-J1 Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug
      DescriptionThe H3K27me3 demethylase inhibitor GSK-J1 (Cat. No. 420204) against JMJD3 and UTX is made cell-permeable by ethyl ester derivatization to facilitate cellular delivery ([medium GSK-J4]t=0 = 30 µM; [cellular GSK-J1]t=1h = 1.6 µM). The pro-drug GSK-J4, being ineffective in cell-free assays, is effectively converted to GSK-J1 intracellularly and inhibits nuclear H3K27me3 levels in both untransfected and JMJD3-transfected HeLa cells (25 to 50 µM). Simultaneous inhibition of cellular JMJD3 and UTX by GSK-J4 treatment is shown to block LPS-induced production of several proinflammatory cytokines, including TNF-α (IC50 = 9 µM by ELISA), in primary human macrophage cultures.
      FormTan semi-solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1373423-53-0
      Chemical formulaC₂₄H₂₇N₅O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesHeinemann, B., et al. 2014. Nature 514 E1.
      Kruidenier, L., et al. 2014. Nature 514, E2.
      Kruidenier, L., et al. 2012. Nature 488, 404.