2. Neuronal Signaling Stem Cell/Wnt PI3K/Akt/mTOR Cytoskeleton Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK
  3. Cholinesterase (ChE) GSK-3 Microtubule/Tubulin ROS Kinase
  4. AChE/GSK-3β-IN-1

AChE/GSK-3β-IN-1 (compound GT15) 是一种有效的双重 AChE/GSK-3β 抑制剂，对 hAChE、hBChE 和 hGSK-3β 的IC50 值分别为 1.2、149.8 和 22.4 nM。AChE/GSK-3β-IN-1 能穿透血脑屏障（BBB）。AChE/GSK-3β-IN-1对 CMGC 激酶家族具有较高的激酶选择性。AChE/GSK-3β-IN-1 占据 DYRK1A 的 ATP 结合位点。AChE/GSK-3β-IN-1 抑制 ROS 表达降低氧化应激。AChE/GSK-3β-IN-1 可用以阿尔兹海默症研究。

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AChE/GSK-3β-IN-1 Chemical Structure

AChE/GSK-3β-IN-1 Chemical Structure

CAS No. : 2412364-73-7

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AChE/GSK-3β-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Cholinesterase (ChE) 亚型特异性产品:

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AChE BChE

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GSK-3 GSK-3α GSK-3β

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research[1].

体外研究
(In Vitro)

AChE/GSK-3β-IN-1 (compound GT15) (300 nM) has strong binding affinities with GSK3 family and exhibits a potent inhibitory activity against dual tyrosine phospho-regulated kinase 1 (DYRK1) (DYRK1α and DYRK1β with IC50 of 28.3 nM and 119.7 nM, respectively)[1].
AChE/GSK-3β-IN-1 (compound GT15) (5-15 µM; 1 hours; N2a-tau cells) exhibits good permeability across the blood-brain-barrier and ability to inhibit the phosphorylation of tau protein[1].
AChE/GSK-3β-IN-1 (compound GT15) (5 µM; BV2 cells) prevents the increase of ROS caused by LPS and reduces oxidative stress[1].

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

AChE/GSK-3β-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: N2a-tau cells
Concentration: 5, 10, and 15 µM
Incubation Time: 6 hours
Result: Decreased the level of phosphorylated tau protein was reduced to 49% at 5 µM and 17% at 15 µM.
体内研究
(In Vivo)

AChE/GSK-3β-IN-1 (compound GT15) (15 mg/kg,; p.o.; ICR male mice) has a function of improving memory and cognition in mice[1].

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

Animal Model: ICR male mice[1]
Dosage: 15 mg/kg
Administration: Oral administration
Result: Improved the cognitive impairment of the mice.
分子量

585.72

Formula

C31H35N7O3S
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

AChE/GSK-3β-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

AChE/GSK-3β-IN-12412364-73-7Cholinesterase (ChE)GSK-3Microtubule/TubulinROS KinaseGlycogen synthase kinase-3Glycogen synthase kinase 3alzheimer’s diseaseglycogen synthase kinase3bacetylcholinesterasemulti-target-directed ligandsInhibitorinhibitorinhibit

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