1. PI3K/Akt/mTOR Stem Cell/Wnt Apoptosis NF-κB
  2. GSK-3 Apoptosis NF-κB c-Myc
  3. GSK-3β-IN-28

GSK-3β inhibitor 28 是一种选择性、非竞争性的糖原合成酶激酶-3β (GSK-3β) 抑制剂,其 IC50 值为 14.82 nM。GSK-3β inhibitor 28 能够上调磷酸化 GSK-3β 的表达水平,下调 p-NF-κBP65C-mycCyclin D1 的表达。GSK-3β inhibitor 28 可诱导细胞凋亡 (apoptosis)、G1 期阻滞并抑制迁移。GSK-3β inhibitor 28 可用于癌症研究,如结直肠癌研究。

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GSK-3β-IN-28

GSK-3β-IN-28 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-3β inhibitor 28 is selective and non-competitivea glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 14.82 nM. GSK-3β inhibitor 28 can upregulate the expression level of phosphorylated GSK-3β and downregulate the expression of p-NF-κB, P65, C-myc and Cyclin D1. GSK-3β inhibitor 28 can induce cells apoptosis, G1 phase arrest and inhibit migration. GSK-3β inhibitor 28 can be used for the research of cancer, such as colorectal cancer[1].

IC50 & Target[1]

GSK-3β

14.82 nM (IC50)

体外研究
(In Vitro)

GSK-3β inhibitor 28 (Compound 7f) 对 SW480、MDA-MB-231 和 A549 细胞表现出较强的抑制活性, IC50 值分别为 14.58、14.61、19.15 μM,而对 MoLM13 细胞 (IC50 = 25.75 μM) 和 HepG2 细胞 (IC50 = 51.51 μM) 的活性较弱[1]
GSK-3β inhibitor 28 (1 μM) 对大多数激酶 (MAPK, EGFR, Src) 具有良好的选择性,但对 GSK-3α 除外,对 GSK-3α 仅表现出中等抑制率 (58.0%)[1]
GSK-3β inhibitor 28 (0.78-25 μM, 72 h) 对 LX-2 (肝星状细胞) 和 MIHA (正常肝细胞) 的 IC50 值均大于 25 μM[1]
GSK-3β inhibitor 28 (5-20 μM, 24 h) 可抑制 SW480 细胞的迁移并减少集落数量[1]
GSK-3β inhibitor 28 (5-20 μM, 24 h) 可诱导 SW480 细胞凋亡并使其停滞在 G1 期[1]
GSK-3β inhibitor 28 (10-20 μM, 72 h) 可上调 SW480 细胞中 p-GSK-3β 的表达,并下调 p-NF-κB,P65、C-myc、Cyclin D1 和 XIAP 蛋白的表达[1]

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

Cell Viability Assay[1]

Cell Line: SW480 cells
Concentration: 5, 10 and 20 μM
Incubation Time: 24 h
Result: Increased proportion of cells in G1 phase.
Decreased proportions in S and G2 phases.
分子量

425.89

Formula

C21H16ClN3O3S

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
GSK-3β-IN-28
目录号:
HY-175850
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