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AG-126
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AG-126图片
CAS NO:118409-62-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
AG-126 是一种酪氨酸激酶抑制剂,可在 25-50 μM 时抑制 ERK1 和 ERK2 的磷酸化。
Cas No.118409-62-4
别名酪氨酸磷酸化抑制剂126,Tyrphostin AG-126
化学名2-[(3-hydroxy-4-nitrophenyl)methylene]-propanedinitrile
Canonical SMILESOC1=C([N+]([O-])=O)C=CC(/C=C(C#N)\C#N)=C1
分子式C10H5N3O3
分子量215.2
溶解度≤0.15mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: inhibits the phosphorylation of ERK1 and ERK2 at 25-50 μM

AG-126 is an ERK1 and ERK2 inhibitor.

Extracellular signal-regulated kinases (ERKs) are widely expressed intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions. Many different stimuli, such as growth factors, cytokines, transforming agents, and carcinogens, can activate the ERK pathway.

In vitro: Previous study found that r AG126 ould potently inhibit the PCW-evoked release and this effect was rather selective with respect to the stimulus. AG126 was found to be less potent in attenuating LPS-triggered release. Moreover, it was found that AG126 was able to prevent the PCW-inducible ERK phosphorylation, which could relate to the AG126-mediated inhibition of PCW-evoked cytokine release [1].

In vivo: AG126 was tested in a model of PCW-induced meningitis, in which rats underwent intracisternal injection of PCW with and without AG126 pretreatment. PCW injection led to a dramatic leukocyte influx into the CSF. AG126 treatment could significantly attenuate such invasion, without changing the number of circulating leukocytes. In addition, AG126 treatment showed beneficial effects on other parameters, such as intracranial pressure. Furthermore, AG126 had no adverse effect on several physiological parameters including mean arterial blood pressure, arterial PaO2, PaCO2 as well as pH [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Hanisch, U. K.,Prinz, M.,Angstwurm, K., et al. The protein tyrosine kinase inhibitor AG126 prevents the massive microglial cytokine induction by pneumococcal cell walls. European Journal of Immunology 31, 2104-2115 (2001).