2. Neuronal Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Stem Cell/Wnt Autophagy Cell Cycle/DNA Damage Cytoskeleton
  3. α-synuclein Bcr-Abl GSK-3 DYRK LRRK2 Microtubule/Tubulin
  4. Dyrk1A-IN-17

Dyrk1A-IN-17 是一种口服有效且能透过血脑屏障的多激酶抑制剂。Dyrk1A-IN-17 通过抑制 ABL1、DYRK1A、GSK3β、LRRK2 四种激酶并稳定微管，进而降低 α-突触核蛋白的过度磷酸化。Dyrk1A-IN-17 可用于帕金森病、阿尔茨海默病等神经退行性疾病的研究。

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Dyrk1A-IN-17

Dyrk1A-IN-17 Chemical Structure

CAS No. : 2201083-51-2

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Dyrk1A-IN-17 相关抗体

Top Publications Citing Use of Products

查看 α-synuclein 亚型特异性产品:

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α-synuclein α-synuclein Aggregation α-synuclein/CHMP2B

查看 Bcr-Abl 亚型特异性产品:

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Abl Bcr-Abl

查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

查看 DYRK 亚型特异性产品:

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dyrk1A-IN-17 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Dyrk1A-IN-17 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Dyrk1A-IN-17 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease[1].

IC50 & Target[1]

GSK-3β

 

Abl1

 

DYRK1A

 

体外研究
(In Vitro)

Dyrk1A-IN-17 (Compound 1) (10 μM) 在体外激酶抑制实验中轻度抑制 ABL1、DYRK1A、GSK3β、LRRK2 四种激酶的活性，平均抑制率分别为 56.5%、48%、61%、59%[1]。
Dyrk1A-IN-17 (100 μM) 可抑制 Colchicine (HY-16569) 与微管蛋白的结合，抑制率为 34%[1]。
Dyrk1A-IN-17 (50 μM) 可抑制 Vinblastine (HY-13780) 与微管蛋白的结合，抑制率为 15%[1]。
Dyrk1A-IN-17 (4-8 μM；10 天) 可在原代大鼠海马细胞培养物中降低 α- 突触核蛋白原纤维诱导的 pSer129 过度磷酸化，细胞核碎片化与固缩程度，以及轻度提升乙酰化 α-微管蛋白水平[1]。

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

Dyrk1A-IN-17 相关抗体:

Immunofluorescence[1]

Cell Line: Primary rat hippocampal cultures treated preformed fibrils
Concentration: 8 μM
Incubation Time: 10 days
Result: Reduced fragmented and condensed
Hoechst+ nuclei in the fibril-treated group.
体内研究
(In Vivo)

Dyrk1A-IN-17 (5 mg/kg；口服) 可适度降低预形成原纤维输注小鼠中枢神经系统中不溶性 α-突触核蛋白的过度磷酸化水平[1]。

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

323.78

Formula

C17H14ClN5
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

Dyrk1A-IN-17 相关分类

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  • 稀释计算器

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Keywords:

Dyrk1A-IN-172201083-51-2α-synucleinBcr-AblGSK-3DYRKLRRK2Microtubule/Tubulinα-SynGlycogen synthase kinase-3Glycogen synthase kinase 3Dual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseLeucine-rich repeat kinase 2BBBprimary neuronsneurodegenerative diseasesmicrotubuleADPDInhibitorinhibitorinhibit

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