ZM336372

An activator of the Raf-1 signalling pathway

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥412.00

330.00

- +
10mg

￥837.00

670.00

- +
50mg

￥2975.00

2380.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

Background

ZM336372 is a potent inhibitor of C-Raf with IC50 value of 70 nM [1]. It is also reported that ZM336372 inhibits SAPK2b/p38β2 with IC50 value of 2 μM.

C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases and plays an important role in the ERK1/2 pathway. It has been reported that abnormal expression of C-Raf correlates with human diseases and also involves in a variety of cancers.

ZM336372 is a potent C-Raf inhibitor and has a different selectivity with the reported C-Raf inhibitor PD98059. When tested with primary neurons, ZM3363372 treatment decreased low potassium-induced apoptosis percent by inhibiting C-Raf activation [2]. In tumor spheroids pretreated with H2O2 and ZM336372 for 24 hours totally abolished the ROS-induced eNOS up-regulation via mediating ERK1/2 signaling pathway [3].

参考文献:
1.? Hall-Jackson, C.A., et al., Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol, 1999. 6(8): p. 559-68.
2.? Burgess, S. and V. Echeverria, Raf inhibitors as therapeutic agents against neurodegenerative diseases. CNS Neurol Disord Drug Targets, 2010. 9(1): p. 120-7.
3.? Wartenberg, M., et al., Reactive oxygen species-mediated regulation of eNOS and iNOS expression in multicellular prostate tumor spheroids. Int J Cancer, 2003. 104(3): p. 274-82.

Protocol

Cell experiment:

Proliferation of H727 and BON cells after treatment with ZM336372 is measured using a 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Cells are trypsinized and plated in triplicate to 24-well plates and allowed to adhere overnight. Then, cells are treated with either 100 μM ZM336372 or DMSO (2%) and incubated. Media are changed every 2 days with new treatment. At each time point, cell growth rates are analyzed after the addition of 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reagent to the cultured cells. Absorbance is determined using spectrophotometer at a wavelength of 540 nm[2].

参考文献:

[1]. Hall-Jackson CA, et al. Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol. 1999 Aug;6(8):559-68.
[2]. Van Gompel JJ, et al. ZM336372, a Raf-1 activator, suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells. Mol Cancer Ther. 2005 Jun;4(6):910-7.