2. 疾病领域
  3. 神经系统疾病
  4. 神经退行性疾病
  5. 亨廷顿病
  6. CAST-calpain-2 stabilizer-1

CAST-calpain-2 stabilizer-1 是一种可穿透血脑屏障的 CAST-calpain-2 相互作用稳定剂。CAST-calpain-2 stabilizer-1 对 GSK3 无活性。CAST-calpain-2 stabilizer-1 可用于亨廷顿病、tau 蛋白病的研究。

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CAST-calpain-2 stabilizer-1

CAST-calpain-2 stabilizer-1 Chemical Structure

CAS No. : 3110929-05-7

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CAST-calpain-2 stabilizer-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

CAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies[1].

体外研究
(In Vitro)

CAST-calpain-2 stabilizer-1 (A36) 可强效恢复 HdhQ111 小鼠纹状体神经元样细胞的线粒体膜电位 (EC50=2.77 μM)，并提高 HdhQ111 小鼠纹状体神经元样细胞的活力(EC50=1.55 μM)[1]。
CAST-calpain-2 stabilizer-1 可上调 HdhQ111 小鼠纹状体神经元样细胞中 CAST 蛋白的表达，EC50 约为 3.55 μM[1]。
CAST-calpain-2 stabilizer-1 可降低 HdhQ111 小鼠纹状体神经元样细胞中的线粒体 ROS 生成，IC50 约为 1.43 μM[1]。
CAST-calpain-2 stabilizer-1 可增强 HdhQ111 小鼠纹状体神经元样细胞中 CAST 与 calpain-2 的内源性相互作用[1]。
CAST-calpain-2 stabilizer-1 (0-500 μM; 40 min) 可在 HdhQ111 小鼠纹状体神经元样细胞裂解液中以剂量依赖的方式直接结合并稳定 CAST 蛋白[1]。
CAST-calpain-2 stabilizer-1 (5-10 μM; 48 h) 需要内源性 CAST 和 calpain-2，才能在 HdhQ111 小鼠纹状体神经元样细胞中发挥线粒体保护及提升细胞活力的作用[1]。
CAST-calpain-2 stabilizer-1 (1 μM; 5 d) 可恢复神经元标志物的表达，抑制 calpain-2 的活性，并挽救人类患者 iPSC 来源的亨廷顿病 (HD) 中型多棘神经元的轴突生长[1]。

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

CAST-calpain-2 stabilizer-1 相关抗体:

Cell Viability Assay[1]

Cell Line: HdhQ111 mouse striatal neuron-like cells
Concentration: 5-10 μM
Incubation Time: 5-10 μM (MTT assay); 48 h (TMRM assay)
Result: Exerted mitochondrial protective and viability-enhancing effects in HdhQ111 mouse striatal neuron-like cell with endogenous CAST and calpain-2.
体内研究
(In Vivo)

CAST-calpain-2 stabilizer-1 (A36) (10 mg/kg，腹腔注射，每周 5 天，持续 6 周) 可恢复 CAST-calpain-2 信号通路，减轻亨廷顿病相关神经病理改变，改善运动功能，并使 R6/2 小鼠在 12 周时的存活率提升 30%[1]。
CAST-calpain-2 stabilizer-1 (10 mg/kg；腹腔注射；每周 5 天；持续 5 个月) 可恢复 CAST-calpain-2 信号通路，减轻与 tau 蛋白病相关的神经病理学改变和神经炎症，并改善 PS19 小鼠的短期及长期记忆[1]。

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

Animal Model: B6;C3Tg (Prnp-MAPT*P301S) PS19 (male, tauopathy model expressing mutant P301S human tau protein)[1]
Dosage: 10 mg/kg
Administration: i.p.; once daily, 5 days per week; 5 months
Result: Improved short-term memory, as shown by enhanced spontaneous alternation performance in the Y maze test.
Improved long-term memory, as shown by reduced escape latency in the Barnes maze test.
Reduced hippocampal phosphorylated tau (AT8-positive) levels.
Reduced neuroinflammation, as shown by decreased IBA1 (microglia) and GFAP (astrocyte) immunodensity in the hippocampus.
Restored hippocampal CAST protein expression and reduced cleavage of calpain-2 substrates (α-spectrin, p35 to p25).
Reduced hippocampal Drp1 phosphorylation at Ser616.
Restored the interaction between endogenous CAST and calpain-2 in hippocampal tissue.
分子量

471.34

Formula

C22H20Cl2N6O2
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

CAST-calpain-2 stabilizer-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

CAST-calpain-2 stabilizer-13110929-05-7OthersCAST proteinhuntington’s diseaseGSK3CAST-calpain-2 complextauopathyp-Drp1 S616human patient iPSC-derived HD medium spiny neuronsHdhQ111 mouse striatal neuron-like cellsR6/2 micecalpain-2Inhibitorinhibitorinhibit

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