1. MAPK/ERK Pathway
  2. JNK
  3. JNK3 inhibitor-8

JNK3 inhibitor-8 是一种有效的、选择性的,具有口服活性并可穿过血脑屏障的 JNK3 抑制剂,对 JNK3、JNK2、JNK1 的 IC50 值分别为 21, 2203, >10000 nM。JNK3 inhibitor-8 显示出显着的神经保护作用。JNK3 inhibitor-8 具有研究阿尔茨海默病 (AD) 的潜力。

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JNK3 inhibitor-8 Chemical Structure

JNK3 inhibitor-8 Chemical Structure

CAS No. : 3034676-53-1

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查看 JNK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD)[1].

IC50 & Target[1]

JNK3

21 nM (IC50)

JNK2

2203 nM (IC50)

JNK1

>10000 nM (IC50)

体外研究
(In Vitro)

JNK3 inhibitor-8 (compound 3h; 10, 20 µM; 24, 48 h) 增加用 10 μM amyloid-β1-42处理的原代大鼠皮层神经元细胞活力[1]
JNK3 inhibitor-8 (10, 20 µM) 降低 p-c-jun (S63)、p-c-jun (S73)、PARP 和 p-Tau 的表达当用10 μM 的 amyloid-β1-42 处理时[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: primary rat cortex neuron cells
Concentration: 10, 20 µM
Incubation Time: 24, 48 h
Result: Increased cell viability when treatment with 10 μM amyloid-β1-42.

Western Blot Analysis[1]

Cell Line: primary rat cortex neuron cells
Concentration: 10, 20 µM
Incubation Time:
Result: Decreased the expression of p-c-jun (S63) and p-c-jun (S73) in 0.5 μM anisomycin or 10 μM amyloid-β1-42 stitumed, and decreased the expression of PARP and p-Tau expression when treatment with 10 μM amyloid-β1-42.
体内研究
(In Vivo)

JNK3 inhibitor-8 (30、60 mg/kg;口服;每日一次,持续 4 周) 对小鼠显示出显着的神经保护作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6 month-old APP/PS1 AD mice[1]
Dosage: 30, 60 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Decrease in escape time and distance traveled, showed a significantly higher level of altered behavioral ability compared to APP/PS1 and vehicle control in the Y-maze test, improved memory and cognitive function.
Animal Model: 10 month-old 3xTg AD mice[1]
Dosage: 30, 60 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Decreased the escape time and the distance, increased TSPQ and TSTZ levels, significantly decreased the expression of pTau levels and improved memory and cognitive function.
分子量

579.62

Formula

C32H30FN7O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

JNK3 inhibitor-8 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JNK3 inhibitor-8
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HY-149280
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