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TCS JNK 6o (Synonyms: JNK Inhibitor VIII)

Catalog No.GC17282

TCS JNK 6o (TCS JNK 6o) is a c-Jun N-terminal kinases (JNK-1, -2, and -3) inhibitor with Ki values of 2 nM, 4 nM, 52 nM, respectively, and has IC50 values of 45 nM and 160 nM for JNK-1 and -2, respectively.

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TCS JNK 6o Chemical Structure

Cas No.: 894804-07-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$149.00
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1mg
$63.00
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5mg
$135.00
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10mg
$225.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 45 nM for JNK1 and 160 nM for JNK2 [1]

TCS JNK 6o is a ATP-competitive and selective c-Jun N-terminal kinase (JNK) inhibitor. JNKs belong to the mitogen-activated protein kinase (MAP kinase) family, and are responsive to stress stimuli, including ultraviolet irradiation, cytokines, osmotic shock and heat shock. JNKs also play a role in the cellular apoptosis and T cell differentiation pathway.

In vitro: CS JNK 6o, in a dose-dependent manner, inhibits phosphorylation of c-jun (EC50 = 920 nM) and prevents collagen-induced platelet aggregation. At low collagen concentrations (0.2 and 0.5 μg/ml), platelet aggregation was totally or partially impaired by 10 μM CS JNK 6o, whereas at a high collagen concentration (5 μg/ml), TCS JNK 6o had no effect [2].

In vivo:. Pharmacokinetic profiles were studied for TCS JNK 6o in Sprague-Dawley rats. TCS JNK 6o showed a short half-life of about 1 hour, with barely measurable bioavailability and rapid clearance. Microsomal incubation studies revealed that the oxidative metabolism of TCS JNK 6o was very rapid [1]

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

References:
[1] Szczepankiewicz BG1, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM.  Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem. 2006 Jun 15;49(12):3563-80.
[2] Kauskot A, Adam F, Mazharian A, Ajzenberg N, Berrou E, Bonnefoy A, Rosa JP, Hoylaerts MF, Bryckaert M.  Involvement of the mitogen-activated protein kinase c-Jun NH2-terminal kinase 1 in thrombus formation. J Biol Chem. 2007 Nov 2;282(44):31990-9.

Chemical Properties

Cas No. 894804-07-0 SDF
Synonyms JNK Inhibitor VIII
Chemical Name N-(4-amino-5-cyano-6-ethoxypyridin-2-yl)-2-(2,5-dimethoxyphenyl)acetamide
Canonical SMILES O=C(CC1=CC(OC)=CC=C1OC)NC2=NC(OCC)=C(C#N)C(N)=C2
Formula C18H20N4O4 M.Wt 356.38
Solubility DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml 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 2.806 mL 14.03 mL 28.0599 mL
5 mM 0.5612 mL 2.806 mL 5.612 mL
10 mM 0.2806 mL 1.403 mL 2.806 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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