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

420204
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420204-10MG
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          Glass bottle 10 mg
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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®
          SynonymsJHDM Inhibitor II, 3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Technical Info

          Title
          White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
          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
          SynonymsJHDM Inhibitor II, 3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid
          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 +2°C to +8°C
          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.
          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.