531996 KDM4A/KDM4B Inhibitor, NSC636819 - Calbiochem

531996
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₁₂Cl₄N₂O₄

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31996.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC50 = 6.4 µM; Ki = 5.5 µM) and KDM4B (IC50 = 9.3 µM; Ki = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC50 = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number531996
          Brand Family Calbiochem®
          SynonymsJMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor
          References
          ReferencesChu, C.H., et al. 2014. Journ. Med. Chem. 57, 5975.
          Product Information
          FormBrown solid
          Hill FormulaC₂₂H₁₂Cl₄N₂O₄
          Chemical formulaC₂₂H₁₂Cl₄N₂O₄
          ReversibleY
          Applications
          Biological Information
          Primary TargetKDM4A/B
          Primary Target K<sub>i</sub>3.0 µ
          Purity≥97% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          KDM4A/KDM4B Inhibitor, NSC636819 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Chu, C.H., et al. 2014. Journ. Med. Chem. 57, 5975.
          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.

          Revision30-January-2017 JSW
          SynonymsJMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor
          DescriptionA cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC50 = 6.4 µM; Ki = 5.5 µM) and KDM4B (IC50 = 9.3 µM; Ki = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC50 = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.
          FormBrown solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₁₂Cl₄N₂O₄
          Purity≥97% by HPLC
          SolubilityDMSO (10 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesChu, C.H., et al. 2014. Journ. Med. Chem. 57, 5975.