2. PI3K/Akt/mTOR Stem Cell/Wnt TGF-beta/Smad
  3. GSK-3 PKA
  4. GSK-3α/β-IN-1

GSK-3α/β-IN-1 是 GSK-3α/β 抑制剂，对 GSK-3α 和 GSK-3β 的 IC50 分别为 0.265 μM 和 0.255 μM。GSK-3α/β-IN-1 也能抑制 PKA，其 IC50 值为 0.188 μM。GSK-3α/β-IN-1 可有效抑制三种胶质母细胞瘤 (GBM) 细胞系的细胞活力（IC50：3-6 μM，72小时），且对人星形胶质细胞无毒性，且代谢稳定性良好。GSK-3α/β-IN-1 在全人血脑屏障 (BBB) GBM 模型中具有潜在的中枢神经系统活性。

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GSK-3α/β-IN-1

GSK-3α/β-IN-1 Chemical Structure

CAS No. : 1574354-24-7

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GSK-3α/β-IN-1 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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PKA PKAR PKACα

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC50 s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC50 : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM[1].

IC50 & Target[1]

GSK-3α

0.265 μM (IC50)

GSK-3β

0.255 μM (IC50)

PKA

0.188 μM (IC50)

体外研究
(In Vitro)

GSK-3α/β-IN-1 (Compound 1) 对 GSK-3α/β 和 PKA 表现出优于其他同源激酶 (CDK2、CDK5、CDK9、ERK1、ERK2、PKBα、PKBβ、PKCα 和 PKCγ) 的激酶选择性[1]。
GSK-3α/β-IN-1 (0.3-300 μM, 24-72 h) 对三种胶质母细胞瘤 (GBM) 细胞系 (U87-MG、T98G 和 U251-MG) 显示出较强的抑制作用，且具有剂量和时间依赖性[1]。
GSK-3α/β-IN-1 (3.3-6.2 μM，72 小时) 显著减少三种细胞系 (U87-MG、U251-MG 和 T98G) G1 期细胞分布，并增加 S 期细胞分布[1]。
GSK-3α/β-IN-1 (6.2 μM，72 小时) 在 GBM 的 BBB 模型中对 BBB 细胞无毒性，并且 BBB 保持完整[1]。
GSK-3α/β-IN-1 的半衰期 (t1/2 为 101 分钟) 比 Verapamil (HY-14275) 高 4 倍以上，且内在清除率较低 (CLint 为 5.6 mL/min/mg/protein)[1]。

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

GSK-3α/β-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: GBM cells (U87-MG, U251-MG, and T98G)
Concentration: 0.3, 1, 3, 10, 30, 100, and 300 μM
Incubation Time: 24, 48, and 72 h
Result: Significantly reduced the cell viability of U87-MG with IC50 15 μM (24h), 4.7 μM (48h) and 3.3 μM (48h).
Significantly reduced the cell viability of U251-MG with IC50 15.1 μM (24h), 8.3 μM (48h) and 6.1 μM (48h).
Significantly reduced the cell viability of T98G with IC50 12 μM (24h), 8.1 μM (48h) and 6.2 μM (48h).

Cell Cycle Analysis[1]

Cell Line: GBM cells
Concentration: U87-MG : 3.3μM, U251-MG : 6.1 μM, T98G : 6.2 μM
Incubation Time: 72 h
Result: Significantly decreased in the cell distribution in G1 phase for all three cell lines at 45.5% (U87-MG), 61.6% (U251-MG), and 65.8% (T98G) and increased in the S phase at 27.8%, 15.9%, and 22.3% respectively.
分子量

343.38

Formula

C21H17N3O2
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-3α/β-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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.

Keywords:

GSK-3α/β-IN-11574354-24-7GSK-3PKAGlycogen synthase kinase-3Glycogen synthase kinase 3Protein kinase ANanomolarInhibitorGBM cellCNSGlioblastomainhibitorinhibit

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