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CAS No.: 1245792-67-9

BCI-215 Catalog No. CSN24804

BCI-215 is a hyperactivator of fibroblast growth factor signaling that is devoid of developmental toxicity and restores defective MAPK activity caused by overexpression of DUSP1 and DUSP6 in mammalian cells. BCI-215 induced rapid and sustained phosphorylation of extracellular signal-regulated kinase (ERK), p38, and c-Jun N-terminal kinase (JNK) in the absence of reactive oxygen species, and its toxicity was partially rescued by inhibition of p38 but not JNK or ERK.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Mitogen-activated protein kinase phosphatases (MKPs) are a subgroup of the dual specificity phosphatase (DUSP) family. DUSP-MKPs dephosphorylate and inactivate the mitogen-activated protein kinases (MAPKs) extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK)/stress-activated protein kinase (SAPK), and p38 on tyrosine and threonine residues, thereby regulating duration and amplitude of mitogenic and survival signaling^[1]. Dusp6 functions as a negative feedback regulator of Fibroblast Growth Factor (FGF) signaling. BCI-215 is a hyperactivator of FGF signaling that is devoid of developmental toxicity and restores defective MAPK activity caused by overexpression of DUSP1 and DUSP6 in mammalian cells. BCI-215 was devoid of cellular toxicity at concentrations up to 50 μM^[2]. In MDA-MB-231 human breast cancer cells, 22 µM of BCI-215 inhibited cell motility, caused apoptosis but not primary necrosis, and sensitized cells to lymphokine-activated killer cell activity^[3].
参考文献

[1] Farooq A, Zhou MM. Structure and regulation of MAPK phosphatases. Cell Signal. 2004;16(7):769–779.
[2] Korotchenko VN, Saydmohammed M, Vollmer LL, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014;15(10):1436–1445.
[3] Kaltenmeier CT, Vollmer LL, Vernetti LA, 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;361(1):39–50.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5232 mL
- 12.6161 mL
- 25.2321 mL
- 5 mM
- 0.5046 mL
- 2.5232 mL
- 5.0464 mL
- 10 mM
- 0.2523 mL
- 1.2616 mL
- 2.5232 mL

技术信息

CAS号

1245792-67-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H22BrNO

运输

蓝冰

分子量

396.32

别名

溶解度

DMSO	30.0 mg/mL (75.7 mM) warming

动物实验配方

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