2. PI3K/Akt/mTOR Stem Cell/Wnt PROTAC
  3. GSK-3 PROTACs
  4. PROTAC GSK-3β Degrader-1

PROTAC GSK-3β Degrader-1 (compound 1) 是靶向 GSK-3β 的降解剂，IC50 为 833 nM。 PROTAC GSK-3β Degrader-1 包含 SB-216763 (GSK-3β 抑制剂), PEG 连接子和 CRBN (E3 连接酶配体)。 PROTAC GSK-3β Degrader-1 降低 Aβ25-35 肽 和 CuSO4 诱导的神经毒性。PROTAC GSK-3β Degrader-1 可用于研究阿尔茨海默病。

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PROTAC GSK-3β Degrader-1 Chemical Structure

PROTAC GSK-3β Degrader-1 Chemical Structure

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PROTAC GSK-3β Degrader-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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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease[1].

IC50 & Target

GSK-3β

833 nM (IC50)

体外研究
(In Vitro)

PROTAC GSK-3β Degrader-1 (1.25-40 μM， 24 h) 在低剂量时，对 SH-SY5Y 的细胞毒性低； 超过 20 μM 时表现出细胞毒性[1]。
PROTAC GSK-3β Degrader-1 (1 μM， 24 h) 在 SH-SY5Y 中抵消 CuSO4 (150 μM) 诱导的神经毒性[1]。
PROTAC GSK-3β Degrader-1 (0.5-1 μM， 2 h) 在 SH-SY5Y 中以剂量依赖性显著降低Aβ25-35 肽诱导的神经毒性[1]。
PROTAC GSK-3β Degrader-1 (0.5-10 μM， 48 h) 在 SH-SY5Y 中以剂量依赖性显著降低 GSK-3β 蛋白水平， DC50为6.22 μM[1]。
PROTAC GSK-3β Degrader-1 (10 μM， 24 h) 在 SH-SY5Y 中通过 UPS 途径降解 GSK-3β 蛋白[1]。

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

PROTAC GSK-3β Degrader-1 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y
Concentration: 0.5 μM, 1 μM
Incubation Time: 2 h, 24 h
Result: Counteracted the neurotoxicity induced by CuSO4 at 1 μM for 24 h.
Reduced the neurotoxicity induced by Aβ25-35 peptide in a dose-dependent manner for 2 h.

Western Blot Analysis[1]

Cell Line: SH-SY5Y
Concentration: 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Decreased GSK-3β protein levels in a dose-dependent manner, with a DC50 value of 6.22 μM.

Western Blot Analysis[1]

Cell Line: SH-SY5Y
Concentration: 10 μM
Incubation Time: 24 h
Result: Had no effect on the total GSK-3β protein level in the presence of lactacystin at a concentration of 5 μM.
分子量

857.73

Formula

C43H42Cl2N6O9
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

PROTAC GSK-3β Degrader-1 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)

质量   浓度   体积   分子量 *
= × ×

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.

Keywords:

PROTAC GSK-3β Degrader-1GSK-3PROTACsGlycogen synthase kinase-3Glycogen synthase kinase 3SH-SY5YPROTACAlzheimer’s diseaseInhibitorinhibitorinhibit

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