1. Signaling Pathways
  2. PI3K/Akt/mTOR
    Stem Cell/Wnt
  3. GSK-3

GSK-3

Glycogen synthase kinase 3 (GSK-3) is a multifunctional serine/threonine kinase found in all eukaryotes. GSK-3 is one of the few signaling mediators that play central roles in a diverse range of signaling pathways, including those activated by Wnts, hedgehog, growth factors, cytokines, and G protein-coupled ligands. GSK-3 targets transcription factors, regulates the activity of metabolic and signaling enzymes, and controls the half-life of proteins by earmarking them for degradation. GSK-3 exists as two isoforms, GSK-3a (51 kDa) and GSK3b (47 kDa), which are encoded by distinct genes. These isoforms often have overlapping functions, but they do not always compensate for each other.

GSK-3 Isoform Specific Products:

  • GSK-3

  • GSK-3α

  • GSK-3β

Cat. No. Product Name Effect Purity
  • HY-10182
    CHIR-99021 Inhibitor 99.76%
    CHIR-99021是 GSK-3α/β 抑制剂,IC50 分别为 10 nM,6.7 nM。 抑制 GSK-3α/β 比同源物 CDC2 和 ERK2 高 500 倍。
  • HY-12012
    SB 216763 Inhibitor 98.01%
    SB 216763是有效,选择性和ATP竞争性的 GSK-3 抑制剂,抑制GSK-3α和GSK-3β的 IC50 为34.3 nM。
  • HY-10590
    TWS119 Inhibitor >98.0%
    TWS119 是一种 GSK-3β 特异性抑制剂,IC50 值为 30 nM,同时可激活 wnt/β-catenin 信号通路。
  • HY-16294
    LY2090314 Inhibitor 99.75%
    LY2090314 是一种有效的 GSK-3 抑制剂,抑制 GSK-3α 和 GSK-3β,IC50 值分别为 1.5 nM 和 0.9 nM。
  • HY-12302
    Kenpaullone Inhibitor 98.07%
    Kenpaullone 是一种有效的 CDK1/cyclin BGSK-3β 抑制剂,IC50 值分别为 0.4 μM 和 23 nM,同时可抑制 CDK2/cyclin A,CDK2/cyclin E 和 CDK5/p25 的活性,IC50 值分别为 0.68 μM,7.5 μM 和 0.85 μM。
  • HY-59090
    1-Azakenpaullone Inhibitor 98.20%
    1-Azakenpaullone (1-Akp) 是具有高度选择性的、ATP 竞争性的糖原合成酶激酶3 β (GSK-3β) 的抑制剂,其IC50 值为 18 nM。
  • HY-128879A
    VP3.15 dihydrobromide Inhibitor 98.22%
    VP3.15 dihydrobromide 是高效、口服生物可利用的,CNS 可渗透的 PDE7-GSK3 双重抑制剂,对PDE7 和GSK3 作用的 IC50 值分别为 1.59 μM 和 0.88 μM。VP3.15 dihydrobromide 具有神经保护和神经修复活性,是多发性硬化症 (MS) 潜在的抗炎和促髓鞘再生联合治疗药物。
  • HY-111380
    EHT 5372 Inhibitor 98.07%
    EHT 5372 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂,其 IC50 值分别为 0.22,0.28 nM。
  • HY-14872
    Tideglusib Inhibitor 99.81%
    Tideglusib (NP031112) 是一种不可逆的 GSK-3 抑制剂,抑制 GSK-3βWTGSK-3βC199AIC50 分别为5 nM,60 nM。
  • HY-10580
    GSK 3 Inhibitor IX Inhibitor 99.66%
    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) 是一种有效的,选择性的,可逆的,ATP 竞争性的 GSK-3α/βCDK1-cyclinB 复合体抑制剂,能够抑制 (GSK-3α/β)/CDK1/CDK5 的活性,IC50 值分别为 5 nM/320 nM/83 nM。
  • HY-10512
    AR-A014418 Inhibitor
    AR-A014418 是一种有效,选择性,ATP 竞争性的 GSK3β 抑制剂,IC50 值为 104 nM。
  • HY-10182B
    CHIR-99021 trihydrochloride Inhibitor
    CHIR-99021 (CT99021) 是一个GSK-3α/β的抑制剂。
  • HY-19807
    Indirubin-3'-monoxime Inhibitor 99.95%
    Indirubin-3'-monoxime 是一种有效的 GSK-3β 抑制剂,对 5-Lipoxygenase 的抑制作用较弱,IC50 值分别为 22 nM 和 7.8-10 µM;Indirubin-3'-monoxime 同时对 CDK5/p25 和 CDK1/cyclin B 也有较强作用,IC50 值分别为 100 和 180 nM。
  • HY-12524
    Bikinin Inhibitor 99.82%
    Bikinin 是一种非甾体类的,植物性 GSK-3/Shaggy-like kinases 的 ATP 竞争性抑制剂,可激活 BR 信号通路。
  • HY-B0320A
    Cromolyn sodium Inhibitor 99.97%
    Cromolyn sodium 是抗过敏化合物。Cromolyn sodium 是一种 GSK-3β 抑制剂,IC50 为 2.0 µM。
  • HY-13862
    AZD1080 Inhibitor 99.10%
    AZD1080 是一种有效的选择性 GSK3 抑制剂。AZD1080 抑制重组人 GSK3αGSK3βpKi (IC50) 分别为 8.2 (6.9 nM) 和 7.5 (31 nM)。
  • HY-15504A
    RGB-286638 free base Inhibitor 98.07%
    RGB-286638 是一种有效的 CDK 抑制剂,抑制 cyclin T1-CDK9cyclin B1-CDK1cyclin E-CDK2cyclin D1-CDK4cyclin E-CDK3p35-CDK5 活性,IC50 分别为 1,2,3,4,5 和 5 nM;同时可抑制 GSK-3β,TAK1,Jak2 和 MEK1,IC50 值分别为 3,5,50,和 54 nM。
  • HY-11012
    TDZD-8 Inhibitor 98.74%
    TDZD-8 是 GSK-3β 的抑制剂,IC50 为 2 μM;TDZD-8 对 Cdk-1/cyclin B,CK-II,PKA 和 PKC 的作用较弱,IC50 值均 >100 μM。
  • HY-10182A
    CHIR-99021 monohydrochloride Inhibitor 99.93%
    CHIR-99021 (CT99021) 是一个GSK-3α/β的抑制剂。
  • HY-12292
    IM-12 Inhibitor
    IM-12 是 GSK-3β 的抑制剂,IC50 值为 53 nM,可增强 Wnt 信号传导。

Glycogen synthase kinase 3 (GSK-3) is a multifunctional serine/threonine kinase found in all eukaryotes. GSK-3 is one of the few signaling mediators that play central roles in a diverse range of signaling pathways, including those activated by Wnt, PI3K, growth factors, cytokines, and ligands for G protein-coupled receptors. The PI3K pathway is known for regulating metabolism, cell growth, and cell survival. The PI3K activity is stimulated by diverse oncogenes and growth factor receptors. PI3K-mediated production of PIP3 leads to the activation of Akt. The activation of Akt leads to the phosphorylation of GSK-3, which is active in resting cells, but is inactivated by the phosphorylation. The GSK-3 has been linked to the regulation of an assembly of transcription factors, including β-catenin, NF-κB, c-Jun, CREB, and STAT. Thus, the altered activity of GSK-3 causes various effects on cytokine expression. 

 

In the absence of Wnt signaling, β-catenin is phosphorylated by CK1 and GSK-3. This phosphorylation leads to recognition by β-TrCP, leading to the ubiquitylation of β-catenin and degradation by the proteasome. Upon binding of a lipid-modified Wnt protein to the receptor complex, a signaling cascade is initiated. LRP is phosphorylated by CK1/CK2 and GSK-3, and Axin is recruited to the plasma membrane. The kinases in the β-catenin destruction complex are inactivated and β-catenin translocates to the nucleus to form an active transcription factor complex with TCF, leading to transcription of a large set of target genes.

 

Some endogenous growth factors could bind to and activate the tyrosine kinase receptor. This facilitates the recruitment of other proteins (SHC, SOS), which results in the activation of the ERK-MAPK cascade and the inhibition of GSK-3. GSK-3 exerts many cellular effects: it regulates cytoskeletal proteins, and is important in determining cell survival/cell death. GSK-3 has also been identified as a target for the actions of lithium. GSK-3 can inhibit glycogen synthase, the enzyme that catalyzes the transfer of glucose from UDPG to glycogen[1][2].

 

Reference:

[1]. Brenner D, et al. Regulation of tumour necrosis factor signalling: live or let die.Nat Rev Immunol. 2015 Jun;15(6):362-74. 
[2]. Conrad M, et al. Regulated necrosis: disease relevance and therapeutic opportunities.Nat Rev Drug Discov. 2016 May;15(5):348-66. 

Isoform Specific Products

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