BCI-215 是一种高效、肿瘤细胞选择性的双重特异性磷酸酶 DUSP-MKP 抑制剂。BCI-215 对肿瘤细胞有细胞毒性，但对正常细胞无毒性。

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.

Solid

DUSP-MKP

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.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Korotchenko VN, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014 Jul 7;15(10):1436-45.
[2]. Kaltenmeier CT, et al. A Tumor Cell-Selective Inhibitor of Mitogen-Activated Protein Kinase Phosphatases Sensitizes Breast Cancer Cells to Lymphokine-Activated Killer Cell Activity. J Pharmacol Exp Ther. 2017 Apr;361(1):39-50.

In Vitro: DMSO : 33.33 mg/mL (84.10 mM; Need ultrasonic)配制储备液