產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg
CAS	522629-08-9
別名
化學(xué)名
分子式	C11H9FN6
分子量	244.23
溶解度	≥ 12.2mg/mL in DMSO
儲(chǔ)存條件	Desiccate at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Mitogen-activated protein (MAP) kinase interacting kinases 1 (MNK1) is a serine/threonine kinase and is able to integrate signal from MAP kinase pathway and phosphorylate eIF4E [1].

CGP 57380 is a specific and selective MNK1 inhibitor. In 293 cells, CGP 57380 (10 μM) inhibited eIF4E phosphorylation in response to fetal calf serum (FCS), arsenite, anisomycin, PMA or tumor necrosis factor alpha. Also, CGP 57380 increased the cap-dependent reporter rluc. In cellular assays, CGP 57380 inhibited eIF4E phosphorylation with IC50 value of 3 μM [1]. In rat vascular smooth muscle cells, CGP 57380 inhibited eIF4E phosphorylation, protein synthesis and VSMC hypertrophy induced by angiotensin II in a dose dependent way [2]. In mouse macrophages, CGP 57380 concentration-dependently inhibited TNFα production stimulated by Escherichia coli lipopolysaccharide (LPS) through posttranscriptional regulation. Also, CGP 57380 inhibited eIF4E phosphorylation. These results suggested that adenine/uridine-rich elements (ARE)-containing TNFα mRNA required eIF4E phosphorylation for initiation of translation [3]. In bone marrow-derived macrophages, CGP 57380 significantly inhibited the production of proinflammatory cytokines monocyte chemoattractant protein-1, TNF and IL-6 [4].

References:

[1]. Knauf U, Tschopp C, Gram H. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol, 2001, 21(16): 5500-5511.

[2]. Ishida M, Ishida T, Nakashima H, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res, 2003, 93(12): 1218-1224.

[3]. Andersson K, Sundler R. Posttranscriptional regulation of TNFalpha expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine, 2006, 33(1): 52-57.

[4]. Rowlett RM, Chrestensen CA, Nyce M, et al. MNK kinases regulate multiple TLR pathways and innate proinflammatory cytokines in macrophages. Am J Physiol Gastrointest Liver Physiol, 2008, 294(2): G452-459.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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