2. Neuronal Signaling MAPK/ERK Pathway NF-κB Apoptosis Stem Cell/Wnt
  3. Tau Protein p38 MAPK NF-κB Apoptosis Bcl-2 Family ERK JNK
  4. Tau Protein Phosphorylation-IN-1

Tau Protein Phosphorylation-IN-1 是一种 tau 蛋白 (tau protein) 磷酸化抑制剂，能有效保护 PC12 细胞免受 Aβ25-35 诱导的细胞毒性 (EC50 = 1.93 μM)，并能穿透血脑屏障。Tau Protein Phosphorylation-IN-1 在体外和体内均能逆转 tau 蛋白的过度磷酸化，显著抑制免疫相关细胞毒性因子的表达，阻断 MAPK 和 NF-κB 信号通路，并显著降低 RAGE 及凋亡 (apoptosis) 因子 Bax/Bcl-2 的表达水平。在阿尔茨海默病小鼠模型中，Tau Protein Phosphorylation-IN-1 可减轻小鼠的神经损伤并改善其学习记忆能力。Tau Protein Phosphorylation-IN-1 适用于阿尔茨海默病的相关研究。

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Tau Protein Phosphorylation-IN-1

Tau Protein Phosphorylation-IN-1 Chemical Structure

CAS No. : 3075165-36-2

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Tau Protein Phosphorylation-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tau Protein Phosphorylation-IN-1 is a tau protein phosphorylation inhibitor that potently protects PC12 cells against Aβ25–35-induced cytotoxicity (EC50 = 1.93 μM), and can penetrate the blood-brain barrier (BBB).Tau Protein Phosphorylation-IN-1 reverses the hyperphosphorylation of tau, significantly inhibits the expression of certain immune-related cytotoxic factors, suppresses the MAPK and NF-κB signaling pathways, and significantly inhibits the expression of RAGE and the apoptosis factors Bax/Bcl-2, both in vitro and in vivo. Tau Protein Phosphorylation-IN-1 relieves nerve damage, and improves learning and memory in an Alzheimer’s disease (AD) mouse model. Tau Protein Phosphorylation-IN-1 can be used for AD research[1].

体外研究
(In Vitro)

Tau Protein Phosphorylation-IN-1 (compound B1) (24 小时) 在 30 μM 浓度下对 PC12 细胞无毒性，在 10 μM 浓度下能显著抵抗 Aβ25-35 诱导的细胞毒性[1]。
Tau Protein Phosphorylation-IN-1 (2.5-10 μM，24 小时) 在 Aβ25-35 诱导的 PC12 细胞中通过多重机制表现出神经保护作用，包括显著降低 Thr181、 Thr205 和 Ser396 位点的 tau 磷酸化水平，抑制 MAPKs (p38、ERK、JNK) 和 NF-κB 的磷酸化，逆转 Aβ 诱导的 iNOS 和 COX-2 表达上调，调控凋亡相关蛋白 Bax/Bcl-2 的表达并抑制 RAGE [1]。

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

Tau Protein Phosphorylation-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Decreased phosphorylated tau levels at Thr181, Thr205, and Ser396 sites caused by Aβ25–35 compared to the model group.
Exhibited stronger inhibition of tau phosphorylation at the Thr181, Thr205, and Ser396 sites than Oleanolic acid (OA)(HY-N0156) or Donepezil (HY-14566) at 10 μM.
Reversed the Aβ25–35-induced upregulation of iNOS and COX-2 levels.
Significantly inhibited RAGE expression at 5 and 10 μM.
Decreased Bax and Bcl-2 expression compared to the control group.
Inhibited the phosphorylation of p38 MAPK, ERK and JNK, thereby blocking the MAPK signaling pathway.
Reduced the expression of p-NF-κB in Aβ25–35-induced PC12 cells.
体内研究
(In Vivo)

Tau Protein Phosphorylation-IN-1 (2.5、5 和 10 mg/kg，腹腔注射，每日一次，持续 28 天) 能够改善阿尔茨海默病小鼠模型中小鼠的认知缺陷，减轻 tau 蛋白过度磷酸化，并抑制神经炎症[1]。

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

Animal Model: Male ICR mice (20-22 g) intracerebroventricularly injected with Aβ₂₅–₃₅ solution (9 nmol/3 μL/mouse) [1]
Dosage: 2.5, 5 and 10 mg/kg
Administration: i.p., daily for 28 days
Result: Reduced the escape latencies on training days 2-5 compared with the Aβ group in the Morris water maze test.
Increased the number of crossings over the original platform location, in contrast to the significant reduction observed in the Aβ group.
Reversed the Aβ-induced histopathological damage, including irregular neuronal distribution and reduced cell numbers in the hippocampal CA1 and CA3 areas.
Significantly reduced the levels of tau phosphorylation at Thr205, and Ser396 sites, compared with the Aβ group.
Significantly decreased the level of tau phosphorylation at the Thr181 site in the hippocampus, especially in the DG, CA1, and CA3 pyramidal neurons.
Suppressed the Aβ25-35-induced upregulation of iNOS, COX-2, RAGE, and the Bax/Bcl-2 ratio.
Showed an inhibitory effect on p38 MAPK, ERK, and JNK phosphorylation in Aβ25-35-induced AD mice.
Inhibited the Aβ25-35-induced upregulation of NF-κB in a dose-dependent manner.
Caused no histopathological damage in the liver or kidneys at any tested dose (up to 10 mg/kg) over 21 days.
分子量

628.89

Formula

C39H56N4O3
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

Tau Protein Phosphorylation-IN-1 相关分类

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Keywords:

Tau Protein Phosphorylation-IN-13075165-36-2Tau Proteinp38 MAPKNF-κBApoptosisBcl-2 FamilyERKJNKNuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesc-Jun N-terminal kinasetau proteinblood-brain barrierAβ25–35-induced PC12 cellshyperphosphorylationMAPKRAGEapoptosisADAβ25–35-induced AD miceInhibitorinhibitorinhibit

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