BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
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Shipped In
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Product Description
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells
In Vitro
BCI-215 concentration-dependently increases pERK levels in DUSP-overexpressing cells with IC 50 value in the micromolar range. BCI-215 (1-20 μM; 6 hours) retains fibroblast growth factor hyperactivating and cellular DUSP6/MKP-3 and DUSP1/MKP-1 inhibitory activity but is nontoxic to zebrafish embryos and an endothelial cell line. BCI-215 inhibits survival and motility of MDA-MB-231 human breast cancer cells but does not affect viability of cultured hepatocytes. BCI-215 is completely devoid of hepatocyte toxicity up to 100 µM. BCI-215 does not generate ROS in hepatocytes or in developing Zebrafish larvae.\nBCI-215 (22 µM) has antimigratory and proapoptotic activities in breast cancer cells that correlate with induction of ERK phosphorylation. BCI-215 (20 µM; 1 hour) induces mitogenic and stress signaling in cancer cells without generating ROS. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: MDA-MB-231 cells Concentration: 22 µM Incubation Time: Result: Caused apoptotic cell death at concentrations that induce ERK phosphorylation. Western Blot AnalysisCell Line: MDA-MB-231 cells Concentration: 20 µM Incubation Time: 1 hour Result: Induced a stress response that is not dependent on oxidation.
Form:Solid
IC50& Target:DUSP-MKP
Associated Targets(non-human)
dusp5-2Dual specificity protein phosphatase (1 Activities)
