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
    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-107531
    A 1070722 Inhibitor
    A 1070722 是一个高效、选择性的糖原合成酶激酶 3 (GSK-3) 抑制剂,对 GSK-3α 和 GSK-3β 作用的 Ki 为 0.6 nM。A 1070722 能穿透血脑屏障并在脑区积聚,具有作为定量测定脑部 GSK-3 的 PET 放射性跟踪剂的潜力。
  • HY-59090
    1-Azakenpaullone Inhibitor >98.0%
    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-108359
    Alsterpaullone Inhibitor
    Alsterpaullone (9-Nitropaullone;NSC 705701) 是一种高效的 CDK 抑制剂,作用于 CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p35 的 IC50 值分别为 35 nM、15 nM、200 nM 和 40 nM。Alsterpaullone 还是 ATP 竞争性 GSK-3alpha/GSK-3beta 抑制剂,IC50 值为 4 nM,具有抗肿瘤活性,有治疗神经退行性和增生性疾病的潜力。
  • 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-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-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-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-15438
    SB 415286 Inhibitor 99.88%
    SB 415286 是一种有效的 GSK-3α 抑制剂,IC50 值为 77.5 nM,Ki 值为 30.75 nM;SB 415286 对人 GSK-3αGSK-3β 的抑制效果相同。
  • 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 99.55%
    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-15761
    AZD2858 Inhibitor 99.24%
    AZD2858 是一种有效的,可口服的 GSK-3 抑制剂,可以抑制 GSK-3αGSK-3β 的活性,IC50 值分别为 0.9 和 5 nM,可用于骨折愈合的研究。

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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