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420204 Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem

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Sinonimi: 3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid, JHDM Inhibitor II

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      Description
      OverviewA pyridinyl-pyrimidinylaminopropanoic acid that effectively inhibits KDM6 family H3K27m3 demethylases JMJD3 and UTX (IC50 = 18 and 56 µM, respectively, by MALDI Mass detection) in an α-ketoglutarate-competitive, peptide substrate-non-competitive manner, displaying much reduced potency against JARID1C, JMJD1a, JMJD2a, JMJD2c, JMJD2d, JMJD2e, as well as112 kinases and 60 non-kinase enzymes. Recommended for cell-free assays only. For culture treatment, use the cell-permeable pro-drug GSK-J4 (Cat. No. 420205).
      Catalogue Number420204
      Brand Family Calbiochem®
      Synonyms3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid, JHDM Inhibitor II
      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 number1373422-53-7
      FormLight yellow powder
      Hill FormulaC₂₂H₂₃N₅O₂
      Chemical formulaC₂₂H₂₃N₅O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetH3K27me3 demethylases JMJD3 & UTX
      Purity≥98% by HPLC
      Physicochemical Information
      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 at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Numero di catalogo GTIN
      420204-10MG 04055977210781

      Documentation

      Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem MSDS

      Titolo

      Scheda di sicurezza (MSDS) 

      Riferimenti bibliografici

      Panoramica delle referenze
      Heinemann, B., et al. 2014. Nature 514 E1.
      Kruidenier, L., et al. 2014. Nature 514, E2.
      Kruidenier, L., et al. 2012. Nature 488, 404.

      Informazioni tecniche

      Titolo
      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
      Scheda tecnica

      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
      Synonyms3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid, JHDM Inhibitor II
      DescriptionA pyridinyl-pyrimidinylaminopropanoic acid that effectively inhibits KDM6 family H3K27me3 demethylases JMJD3 (IC50 = 0.06 and 18 µM, respectively, by AlphaScreen and MALDI Mass detection method) and UTX (IC50 = 56 µM by MALDI Mass detection) in a α-ketoglutarate-competitive, peptide substrate-non-competitive manner, displaying much reduced potency against JARID1C, JMJD1a, JMJD2a, JMJD2c, JMJD2d, JMJD2e, 112 kinases, as well as a panel of 60 non-kinase enzymes, GPCRs, ion channels, nuclear receptors, and transporters. Recommended for cell-free assays only. For culture treatment, use the cell-permeable pro-drug GSK-J4 (Cat. No. 420205). Structural analysis reveals that the effective inhibition is a result of concerted action of GSK-J1 against the bindings of α-ketoglutarate, histone H3, as well as Fe+2 at the enzyme active site.
      FormLight yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1373422-53-7
      Chemical formulaC₂₂H₂₃N₅O₂
      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 at -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.