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.
IC50&Target
DUSP-MKP
体外研究
BCI-215 concentration-dependently increases pERK levels in DUSP-overexpressing cells with IC50 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.
Apoptosis Analysis
Cell Line:
MDA-MB-231 cells
Concentration:
22 µM
Incubation Time:
Result:
Caused apoptotic cell death at concentrations that induce ERK phosphorylation.
Western Blot Analysis
Cell Line:
MDA-MB-231 cells
Concentration:
20 µM
Incubation Time:
1 hour
Result:
Induced a stress response that is not dependent on oxidation.
分子式
C22H22BrNO
分子量
396.32
CAS号
1245792-67-9
运输条件
Room temperature in continental US; may vary elsewhere.