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. BCI-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
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BCI-215
CAS number：1245792-67-9 molecular formula：C22H22BrNO
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| Chinese alias | - | ||
| English alias | (2E)-2-benzylidene-5-bromo-3-(cyclohexylamino)-3H-inden-1-one | 1245792-67-9 | 1H-Inden-1-one, 5-bromo-3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-, (2E)- | D81258 | HY-121087 | BCI-215 | SCHEMBL6984391 | C22H22BrNO | DTXSID701135398 | EX-A3609 | | ||
| CAS number | 1245792-67-9 | molecular formula | C22H22BrNO |
| molecular weight | 396.3 g/mol | Exact mass | ≥99% |
| PSA | 29.100 Ų | logp | 5.400 |
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