531996 KDM4A/KDM4B Inhibitor, NSC636819 - Calbiochem

531996
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₁₂Cl₄N₂O₄

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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
      Quality LevelMQ100
      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.