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

420205
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420205-10MG
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          Glass bottle 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®
          SynonymsJHDM Inhibitor II Pro-Drug, 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
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          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 Pro-Drug, 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
          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 +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 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.