2. MAPK/ERK Pathway
  3. JNK
  4. JNK3 inhibitor-4

JNK3 inhibitor-4 是一种强效 JNK3 抑制剂 (IC50=1.0 nM)，是基于 2-芳基-1-嘧啶基-1H-咪唑-5-基乙腈的化合物。JNK3 inhibitor-4 对其他蛋白激酶具有极好的选择性，包括同种型 JNK1 (IC50=143.9 nM) 和 JNK2 (IC50=298.2 nM)。JNK3 inhibitor-4 具有神经保护作用和预测的血脑屏障通透性。

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JNK3 inhibitor-4 Chemical Structure

JNK3 inhibitor-4 Chemical Structure

CAS No. : 2409109-65-3

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JNK3 inhibitor-4 相关抗体

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查看 JNK 亚型特异性产品:

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JNK1 JNK2 JNK3 JNK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNK3 inhibitor-4 is a potent inhibitor of JNK3 (IC50=1.0 nM) based on 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile. JNK3 inhibitor-4 shows excellent selectivity over other protein kinases including isoforms JNK1 (IC50=143.9 nM) and JNK2 (IC50=298.2 nM)[1]. JNK3 inhibitor-4 has neuroprotective effect and predicated blood-brain barrier permeability[1].

IC50 & Target[1]

JNK3

1.0 nM (IC50)

JNK1

143.9 nM (IC50)

JNK2

298.2 nM (IC50)

体外研究
(In Vitro)

JNK3 inhibitor-4 (化合物 15d) (1,5,10,20 μM; 24 h 或 48 h) 抑制 Aβ1-42 诱导的对大鼠原代皮层神经元的细胞毒性[1]。
JNK3 inhibitor-4 (10, 20 μM; 24 h、48 h) 抑制 10 μM Aβ1-42 或 0.5 μM Anisomycin (HY-18982) 诱导的大鼠皮层神经元 c-jun 磷酸化和 APP 磷酸化[1]。
JNK3 inhibitor-4 (50 μM; 4 h) 在 Caco-2 试验中具有高渗透性，根据 PAMPA 试验中的有效渗透系数 (Pe) > 4，预测其具有血脑屏障 (CNS+) 渗透性[1]。
JNK3 inhibitor-4 也抑制 GSK3α (h)、GSK3β (h)、JNK1、2、MKK6、MOK、SAPK2a (h)、SAPK2a (T106 M) (h)、SAPK2b (h)、MKK4、JNK1α1 (h) 和JNK2α1 (h)，其 IC50 值分别为 5.78、11.7、15.1、1.18、3.10、1.19、0.280、0.970、0.860 和 0.340 μM[1]。

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

JNK3 inhibitor-4 相关抗体:

Western Blot Analysis[1]

Cell Line: Primary rat cortex neuron
Concentration: 10 μM and 20 μM
Incubation Time: 24 hours
Result: Monomeric Aβ1-42 induced c-jun phosphorylation dose-dependently and that was inhibited by JNK3 inhibitor-4 in concentration-dependent manner.

Cell Viability Assay[1]

Cell Line: Primary rat cortex neuron
Concentration: 1, 5, 10, 20 μM
Incubation Time: 24 hours and 48 hours
Result: Showed neuroprotective effect and increased cell viability under Aβ1-42 treatment.
体内研究
(In Vivo)

JNK3 inhibitor-4 (化合物 15d) 能够改善阿尔茨海默病模型小鼠的记忆力。JNK3 inhibitor-4 (10 mg/kg 或 30 mg/kg; 静脉注射; 每周 3 次，共 1 个月) 在 Y 迷宫试验和被动回避试验中，与 APP/PS1 载药组相比，显著改善了小鼠的自发改变和反应延迟行为 (第 27 天或第 30 天)，并表现出剂量相关性[1]。
JNK3 inhibitor-4 (30 mg/kg; 静脉注射; 单剂量; 记录 0-6 h) 在 SD 大鼠中显示血脑屏障通透性，脑/血浆浓度比为 0.02 (26 ng/g vs 1084 ng/mL)[1]。
Pharmacokinetics in rats[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) BA (%)
IV 1 718.0 0.22
PO 3 337.5 377.82 0.63 0.34 15.67

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

477.56

Formula

C28H27N7O
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-4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

JNK3 inhibitor-42409109-65-3JNKc-Jun N-terminal kinaseAlzheimer’s diseaseInhibitorinhibitorinhibit

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