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Beschreibung

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