2. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage
  3. GSK-3 CDK
  4. GSK-3 inhibitor 4

GSK-3 inhibitor 4 是一种具有口服活性和脑渗透性的 GSK-3，CDK2 和 CDK5的抑制剂，IC50 值分别为 0.56 nM (GSK-3β)，0.45 nM (GSK-3α)，0.47 μM，0.68 μM。GSK-3 inhibitor 4 能有效降低 Tau protein 水平。GSK-3 inhibitor 4 可用于阿尔茨海默症的研究 (AD)。

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GSK-3 inhibitor 4 Chemical Structure

GSK-3 inhibitor 4 Chemical Structure

CAS No. : 2227279-83-4

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GSK-3 inhibitor 4 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

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies[1].

IC50 & Target

GSK-3α

0.45 nM (IC50)

GSK-3β

0.56 nM (IC50)

CDK2

0.47 μM (IC50)

CDK5

0.68 μM (IC50)

体外研究
(In Vitro)

GSK-3 inhibitor 4 (compound 40) 对 CDK2 (840-fold, IC50 = 0.47 μM)，CDK5 (1200-fold, IC50 = 0.68 μM)，GSK-3β (IC50 = 0.56 nM)，和 GSK-3α (IC50 = 0.45 nM) 表现出极佳的选择性[1]。
GSK-3 inhibitor 4具有良好的渗透性，由于其亲脂性，表现出与血浆蛋白和脑组织结合的高能力[1]。

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

GSK-3 inhibitor 4 相关抗体:
体内研究
(In Vivo)

GSK-3 inhibitor 4 (10 mg/kg, p.o.) 当以 10 mg/kg 的剂量口服纳米悬浮液时，pTau396 减少 37%[1]。
GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) 表现出低-中度的清除率，从 15.8 到 23.3 mL/min/kg，以溶液形式口服时吸收良好[1]。

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

Animal Model: 3xTg mice were bred onto the C57BL6 background and bred as homozygotes. Male animals between the ages of five to seven months were used for the study[1].
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.)
Result: Produced a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg.
Animal Model: male C57BL6 mice (Pharmacokinetic assay)[1]
Dosage: 2 mg/kg, 10 mg/kg.
Administration: Kept for 8 h fasting prior to formulation administration. intravenous and oral routes of administration to mice at a dose of 2 and 10 mg/kg, respectively.
Result: Exhibited clearance ranging from 15.8 to 23.3 mL /min/kg , halflives ranging from 2.5 to 2.9 h and were readily orally bioavailable (F% = 53).
分子量

403.38

Formula

C22H15F2N5O
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-3 inhibitor 4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

GSK-3 inhibitor 42227279-83-4GSK-3CDKGlycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseGSK-3βGSK-3αCDK2CDK5GSK-3 inhibitorU2OSAlzheimer's diseaseADInhibitorinhibitorinhibit

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