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531996 KDM4A/KDM4B Inhibitor, NSC636819 - CAS 1618672-71-1 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1618672-71-1C₂₂H₁₂Cl₄N₂O₄

Products

Catalog NumberPackaging Qty/Pack
5.31996.0001 Glass bottle 10 mg
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
CAS number1618672-71-1
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
Global Trade Item Number
Catalog Number GTIN
5.31996.0001 04055977287134

Documentation

KDM4A/KDM4B Inhibitor, NSC636819 - CAS 1618672-71-1 - 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
CAS number1618672-71-1
Chemical formulaC₂₂H₁₂Cl₄N₂O₄
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
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.