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CAS No.: 894804-07-0

JNK Inhibitor VIII Catalog No. CSN23162

Synonyms: TCS JNK 6o;c-Jun N-terminal Kinase Inhibitor VIII

JNK Inhibitor VIII (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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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述c-Jun N-terminal kinase-1 (JNK-1) is a member of the mitogen activated protein kinase (MAP kinase) family of enzymes responsible for the serine/threonine phosphorylation of intracellular targets. JNK-1 and the other JNK enzymes JNK-2 and JNK-3 are activated in response to cellular stresses and various cytokines, and they participate in the onset of apoptosis. TCS JNK 6o is a pan-JNK inhibitor with K_i values of 2, 4 and 52 nM for JNK-1, JNK-2 and JNK-3, respectively, and has IC₅₀ values of 45 and 160 nM for JNK-1 and JNK-2, respectively. In Sprague-Dawley rats, TCS JNK 6o showed a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism was very rapid with this compound^[2]. Moreover, inhibition of primordial follicle activation occurred in the presence of TCS JNK 6o when compared with controls (P < 0.05) after 2 days of culture^[3].
参考文献

[1] Szczepankiewicz BG, et al. 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] Szczepankiewicz BG, Kosogof C, Nelson LT, et al. Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem. 2006;49(12):3563-3580
[3] Bertoldo MJ, Bernard J, Duffard N, et al. Inhibitors of c-Jun phosphorylation impede ovine primordial follicle activation. Mol Hum Reprod. 2016;22(5):338-349

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8060 mL
- 14.0301 mL
- 28.0603 mL
- 5 mM
- 0.5612 mL
- 2.8060 mL
- 5.6121 mL
- 10 mM
- 0.2806 mL
- 1.4030 mL
- 2.8060 mL

技术信息

CAS号

894804-07-0

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H20N4O4

运输

蓝冰

分子量

356.38

别名

TCS JNK 6o;c-Jun N-terminal Kinase Inhibitor VIII

溶解度

DMSO	69.0 mg/mL (193.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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