2. PI3K/Akt/mTOR Stem Cell/Wnt Neuronal Signaling JAK/STAT Signaling TGF-beta/Smad Epigenetics
  3. GSK-3 Tau Protein AAK1 Pim PKC
  4. GSK-3β inhibitor 13

GSK-3β inhibitor 13 (compound 47) 是一种具有口服活性且有效的 GSK-3β 抑制剂，具有血脑通透性。GSK-3β inhibitor 13 抑制 GSK-3β 和 GSK-3α，IC50 分别为 0.73 nM 和 0.35 nM。GSK-3β inhibitor 13 显着降低 tau 的磷酸化 (IC50=58 nM)，而磷酸化的 tau 会引起与阿尔茨海默相关的神经原纤维缠结的形成。

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GSK-3β inhibitor 13 Chemical Structure

GSK-3β inhibitor 13 Chemical Structure

CAS No. : 2227316-74-5

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GSK-3β inhibitor 13 相关抗体

Top Publications Citing Use of Products

查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

查看 Pim 亚型特异性产品:

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PIM1 PIM2 PIM3

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

0.73 nM (IC50)

GSK-3α

0.35 nM (IC50)

PKCθ

0.36 μM (IC50)

PIM1

0.38 μM (IC50)

AAK1

0.20 μM (IC50)

体内研究
(In Vivo)

GSK-3β inhibitor 13 在血浆中的暴露量为 3.8 μM，在脑中的暴露量为 1.3 μM，导致脑-血浆 (B/P) 比率为 0.34[1]。
GSK-3β inhibitor 13 (30 mg/kg；口服；单剂量) 在 LaFerla 3xTg-C57BL6 小鼠中降低 52% 的 pTau396 水平[1]。

在小鼠中的药代动力学分析[1]

Route Dose (mg/kg) CL (mL/mL/kg) Vss (L/kg) MRT (h) t1/2 (h)
i.v. 2 3.8 1.1 4.8 5.2
Route Dose (mg/kg) AUCtot (μM·h) Cmax (μM) F (%)
p.o. 10 68.3 7.8 64

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

414.46

Formula

C23H22N6O2
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

GSK-3β inhibitor 13 相关分类

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Keywords:

GSK-3β inhibitor 132227316-74-5GSK-3Tau ProteinAAK1PimPKCGlycogen synthase kinase-3Glycogen synthase kinase 3Adaptor-associated Kinase 1AP2-associated kinase 1Pim kinasesProtein kinase CInhibitorinhibitorinhibit

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