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A 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.
Chu, C.H., et al. 2014. Journ. Med. Chem.57, 5975.
数据表
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.
A 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.
Form
Brown solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1618672-71-1
Chemical formula
C₂₂H₁₂Cl₄N₂O₄
Purity
≥97% by HPLC
Solubility
DMSO (10 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Chu, C.H., et al. 2014. Journ. Med. Chem.57, 5975.
