TCS JNK 6o
(Synonyms: JNK Inhibitor VIII) 目录号 : GC17282
A JNK inhibitor
Cas No.:894804-07-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 别名 | JNK Inhibitor VIII | ||
| 化学名 | 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 | ||
| 分子式 | C18H20N4O4 | 分子量 | 356.38 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。