2. Stem Cell/Wnt PI3K/Akt/mTOR Cell Cycle/DNA Damage Epigenetics Neuronal Signaling
  3. GSK-3 HDAC Tau Protein
  4. GSK-3β/HDAC-IN-2

GSK-3β/HDAC-IN-2 是一种强效的 GSK-3β 抑制剂 (IC50 为 0.04 μM)、HDAC2 (IC50 为 1.05 μM，Ki 为 0.070 μM)，和 HDAC6 抑制剂 (IC50 为 1.52 μM，Ki 为 0.017 μM)。GSK-3β/HDAC-IN-2 抑制 HDAC2 和 HDAC6 的活性，并阻止 tau 蛋白的过度磷酸化。GSK-3β/HDAC-IN-2 展现出神经保护作用且无明显的毒性。GSK-3β/HDAC-IN-2 可用于阿尔兹海默症的研究。

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GSK-3β/HDAC-IN-2

GSK-3β/HDAC-IN-2 Chemical Structure

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GSK-3β/HDAC-IN-2 相关抗体

Top Publications Citing Use of Products

查看 GSK-3 亚型特异性产品:

查看所有亚型
GSK-3 GSK-3α GSK-3β

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

0.04 μM (IC50)

HDAC6

1.52 μM (IC50)

HDAC2

1.05 μM (IC50)

HDAC6

0.017 μM (Ki)

HDAC1

0.036 μM (Ki)

HDAC3

0.066 μM (Ki)

HDAC2

0.070 μM (Ki)

HDAC8

0.772 μM (Ki)

体外研究
(In Vitro)

GSK-3β/HDAC-IN-2 (Compound 19) 在 15 μM 浓度下对 GSK-3β、HDAC2 和 HDAC6 表现出优异的抑制水平，抑制率分别为 100%，86.51% 和 88.60%[1]。

GSK-3β/HDAC-IN-2 (0.1-100 μM, 24 h) 无明显细胞毒性，且在较低浓度 (0.1 μM) 下可以诱导细胞增殖[1]。

GSK-3β/HDAC-IN-2 (10 μM, pretreated with 1 h and then co-incubated for 16 h) 完全抵消了硫酸铜 (400 μM, 16 h) 诱导的分化型 SH-SY5Y 细胞中 tau 蛋白磷酸化[1]。

GSK-3β/HDAC-IN-2 (0.5 μM, 24 h) 减轻了 SH-SY5Y 细胞中硫酸铜 (600 μM) 导致的 (600 μM) 的神经毒性[1]。

GSK-3β/HDAC-IN-2 (0.1-10 μM, 24 h) 诱导磷酸化 GSK-3β (Ser9) 水平以及 histone H3 和 tubulin 的乙酰化水平[1]。

GSK-3β/HDAC-IN-2 在 SH-SY5Y 细胞中通过染色质重塑、组蛋白调节和细胞周期检查点破坏，选择性地诱导有丝分裂应激反应中的细胞凋亡[1]。

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

GSK-3β/HDAC-IN-2 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1, 10, 25, 50, and 100 μM
Incubation Time: 24 h
Result: Showed no significant cytotoxicity at 100 μM and induced cell proliferation at a lower concentration (0.1 μM).

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells incubated with CuSO4 (600 μM) for 24 h
Concentration: 0.5 μM
Incubation Time: 24 h, co-incubated with CuSO4 (600 μM)
Result: Displayed a significant ability to reduce the CuSO4 neurotoxicity with a neuroprotective activity of 96.1%.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in phospho-GSK-3β (Ser9) levels.
Induced a massive dose-dependent increase in the acetylation levels of both histone H3 and tubulin, starting from the concentration of 1 μM.
分子量

337.31

Formula

C12H11N5O5S
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/HDAC-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

GSK-3β/HDAC-IN-2GSK-3HDACTau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3Histone deacetylasesAlzheimer’s disease (AD)Glycogen Synthase Kinase 3β (GSK-3β)Histone Deacetylases (HDACs)HDAC2HDAC6SH-SY5Y cellsInhibitorinhibitorinhibit

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