TCS JNK 6o (Synonyms: JNK Inhibitor VIII) |
Catalog No.GC17282
One-Click Copy Product Info
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TCS JNK 6o (TCS JNK 6o) est un inhibiteur des kinases N-terminales c-Jun (JNK-1, -2 et -3) avec des valeurs Ki de 2 nM, 4 nM, 52 nM, respectivement, et a des valeurs IC50 de 45 nM et 160 nM pour JNK-1 et -2, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 894804-07-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 894804-07-0 | SDF | |
| Synonymes | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.806 mL | 14.03 mL | 28.0599 mL |
| 5 mM | 561.2 μL | 2.806 mL | 5.612 mL |
| 10 mM | 280.6 μL | 1.403 mL | 2.806 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)