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[1]。

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GSK-3β/HDAC-IN-2 Chemical Structure

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]

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

The molarity calculator equation

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

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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