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JNK3 inhibitor-4
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JNK3 inhibitor-4
CAS No. : 2409109-65-3
MCE 站:JNK3 inhibitor-4
产品活性: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。
研究领域:MAPK/ERK Pathway
作用靶点:JNK
In Vitro: JNK3 inhibitor-4 (compound 15d) (1, 5, 10, 20 μM; 24 h and 48 h) inhibits Aβ1-42 induced Aβ1-42-induced cellular toxicity in primary rat cortex neuron.
JNK3 inhibitor-4 (10 μM and 20 μM; 24 h and 48 h) inhibits c-jun phosphorylation and APP phosphorylation induced by 10 μM Aβ1-42 or 0.5 μM Anisomycin (HY-18982) in primary rat cortex neuron.
JNK3 inhibitor-4 (50 μM; 4 h) shows high permeability in Caco-2 assay and is predicted as BBB permeable (CNS+) based on effective permeability coefficient (Pe) value > 4 in PAMPA assay.
JNK3 inhibitor-4 also shows inhibitory potency on GSK3α (h), GSK3β (h), JNK1, 2, MKK6, MOK, SAPK2a (h), SAPK2a (T106 M) (h), SAPK2b (h), MKK4, JNK1α1 (h), and JNK2α1 (h). These shows IC50 values of 5.78, 11.7, 15.1, 1.18, 3.10, 1.19, 0.280, 0.970, 0.860, and 0.340 μM, respectively.
In Vivo: JNK3 inhibitor-4 improves memory for the Alzheimer’s disease mouse model. JNK3 inhibitor-4 (compound 15d) (10 or 30 mg/kg; i.v.; 3 times/week for 1 month in 9-month-old APP/PS1 3Tx3Tg mice) results significantly higher spontaneous alteration and response latency of mouse (at 27th or 30th days) compared to the APP/PS1vehicle groups in Y-maze test and passive avoidance test, with a dose correlation.
JNK3 inhibitor-4 (30 mg/kg; p.o.; single dose) shows blood-brain barrier permeability with brain to plasma ratio of 0.02 in SD rats.
Pharmacokinetics in rats
Route | Dose (mg/kg) | AUC0-t (ngh/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 |
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