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Beschreibung

A cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR, Ki = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs. Displays dose-dependent binding to full-length HuR protein and to RRM1/2 fragment. Exhibits cytotoxicity towards tumor cells and reduces their viability (IC50 = 28.9 and 18.2 µ,M for HCT-116 and MioPaCa2 cells, respectively). Has much reduced effect on normal WI-38 and CCD 841 CoN cells. Shown to induce cleavage of poly (ADP-ribose) polymerase and pro-caspase 3 (~ 50 µ,M) and reduce the half-life of Bcl-2, Msi1, and XIAP in HCT-116 cells (~20 µ,M) treated with actinomycin D (5 µ,g/ml).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., A cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR, Ki = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs. Displays dose-dependent binding to full-length HuR protein and to RRM1/2 fragment. Exhibits cytotoxicity towards tumor cells and reduces their viability (IC50 = 28.9 and 18.2 µ,M for HCT-116 and MioPaCa2 cells, respectively). Has much reduced effect on normal WI-38 and CCD 841 CoN cells. Shown to induce cleavage of poly (ADP-ribose) polymerase and pro-caspase 3 (~ 50 µ,M) and reduce the half-life of Bcl-2, Msi1, and XIAP in HCT-116 cells (~20 µ,M) treated with actinomycin D (5 µ,g/ml).