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

509453
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Key Spec Table

Empirical FormulaCAS #
C₁₇H₁₃ClN₄ 199596-05-9

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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
      Quality LevelMQ100
      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

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

      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
      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.