509453 JHDM Inhibitor VII, JIB-04 - CAS 199596-05-9 - Calbiochem

509453
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₃ClN₄ 199596-05-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09453.0001
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          Glass bottle 10 mg
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          Description
          OverviewThe E-isomer of a cell-permeable pyridine hydrazone compound that acts as a selective inhibitor against Jumonji family histone demethylases (IC50 = 230, 290-320, 340, 435, 445, 855, and 1,100 nM, respectively, against JARID1A/KDM5A, JMJD2D/KDM4D, JMJD2E/KDM4E, JMJD2B/KDM4B, JMJD2A/KMD4A, JMJD3/KDM6B, and JMJD2C/KDM4C, respectively), presumably via catalytic site iron interaction, displaying little toward 5mC DNA hydroxylase TET1, aurora kinases, HDACs, HIF prolyl hydroxylase PHD2, histone methyltransferases, protein arginine methyltransferases, sirtuins, or the non-jumonji family histone demethylase LSD1/KDM1A. Shown to exhibit anticancer activity against H358 and A549 lunger cancer cells both in cultures in vitro (IC50 in 4 d = 100 and 250 nM, respectively) and in mice in vivo (via i.p. at 100 mg/kg and p.o. at 55 mg/kg, respectively; 2-3 times per week).
          Catalogue Number509453
          Brand Family Calbiochem®
          Synonyms5-Chloro-2-((2E)-2-(phenyl(2-pyridinyl)methylene)hydrazino)pyridine, Histone Lysine Demethylase Inhibitor XIII, NSC693627, JIB04
          References
          ReferencesWang, L., et al. 2013. Nat. Commun. 4, 2035.
          Product Information
          CAS number199596-05-9
          FormLight beige solid
          Hill FormulaC₁₇H₁₃ClN₄
          Chemical formulaC₁₇H₁₃ClN₄
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Target Jumonji family of histone demethylases
          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 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
          Wang, L., et al. 2013. Nat. Commun. 4, 2035.

          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.

          Revision21-February-2014 JSW
          Synonyms5-Chloro-2-((2E)-2-(phenyl(2-pyridinyl)methylene)hydrazino)pyridine, Histone Lysine Demethylase Inhibitor XIII, NSC693627, JIB04
          DescriptionThe (E)-isomer of a cell-permeable pyridine hydrazone compound that acts as a selective inhibitor against Jumonji family histone demethylases (IC50 = 230, 290-320, 340, 435, 445, 855, and 1,100 nM, respectively, against JARID1A/KDM5A, JMJD2D/KDM4D, JMJD2E/KDM4E, JMJD2B/KDM4B, JMJD2A/KMD4A, JMJD3/KDM6B, and JMJD2C/KDM4C, respectively), presumably via catalytic site iron interaction, displaying little or no potency toward 5mC DNA hydroxylase TET1, aurora kinases, HDACs, HIF prolyl hydroxylase PHD2, histone methyltransferases, protein arginine methyltransferases, sirtuins, or the non-jumonji family histone demethylase LSD1/KDM1A. Shown to exhibit anticancer activity against H358 and A549 lunger cancer cells both in cultures in vitro (IC50 = 100 and 250 nM, respectively, in 4 d by MTS assays) and in mice in vivo (via i.p. at 100 mg/kg and p.o. at 55 mg/kg, respectively; 2-3 times per week).
          FormLight beige solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number199596-05-9
          Chemical formulaC₁₇H₁₃ClN₄
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          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
          ReferencesWang, L., et al. 2013. Nat. Commun. 4, 2035.