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AG-126 (Synonyms: Tyrphostin AG-126)

カタログ番号GC17265

AG-126 はチロシンキナーゼ阻害剤であり、25 ~ 50 μM で ERK1 および ERK2 のリン酸化を阻害できます。

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AG-126 化学構造

Cas No.: 118409-62-4

サイズ 価格 在庫数 個数
5mg
$57.00
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10mg
$97.00
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25mg
$233.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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).

Chemical Properties

Cas No. 118409-62-4 SDF
同義語 Tyrphostin AG-126
Chemical Name 2-[(3-hydroxy-4-nitrophenyl)methylene]-propanedinitrile
Canonical SMILES OC1=C([N+]([O-])=O)C=CC(/C=C(C#N)\C#N)=C1
Formula C10H5N3O3 M.Wt 215.2
溶解度 ≤0.15mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.6468 mL 23.2342 mL 46.4684 mL
5 mM 0.9294 mL 4.6468 mL 9.2937 mL
10 mM 0.4647 mL 2.3234 mL 4.6468 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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