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

GSK-3 (糖原合成酶激酶3)

Glycogen synthase kinase-3; Glycogen synthase kinase 3

Glycogen synthase kinase 3 (GSK-3) is a multifunctional serine/threonine kinase consisting of two isoforms, alpha and beta. It is a highly conserved negative regulator of receptor tyrosine kinase, cytokine, and Wnt signaling pathways. Stimulation of these pathways inhibits GSK-3 to modulate diverse downstream effectors that include transcription factors, nutrient sensors, glycogen synthesis, mitochondrial function, circadian rhythm, and cell fate. GSK-3 also regulates alternative splicing in response to T-cell receptor activation, and recent phosphoproteomic studies have revealed that multiple splicing factors and regulators of RNA biosynthesis are phosphorylated in a GSK-3-dependent manner.

The malfunction or aberrant activity of GSK-3 leads to several of disorders, such as Alzheimer's disease (AD) and other neurodegenerative pathologies, and other type of diseases as diabetes, cardiovascular disorders and cancer. GSK-3 is also related to innate immune response against pathogens, which makes GSK-3 an excellent target for therapeutic intervention.

GSK-3 亚型特异性产品:

GSK-3 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10182
    Laduviglusib Inhibitor 99.76%
    Laduviglusib (CHIR-99021) 是一种有效的，选择性的，具有口服活性的 GSK-3α/β 抑制剂，IC50 为 10 nM 和 6.7 nM。Laduviglusib 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib 能诱导细胞自噬 (autophagy)。
    Laduviglusib
  • HY-12012
    SB 216763 Inhibitor 99.82%
    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。
    SB 216763
  • HY-13867
    Bisindolylmaleimide I Inhibitor 98.66%
    Bisindolylmaleimide I (GF109203X) 是一种具有细胞渗透性和可逆性的 PKC 抑制剂 (对 PKCα, PKCβI, PKCβII, and PKCγ 的 IC50 分别为 20 nM、17 nM、16 nM 和 20 nM)。 Bisindolylmaleimide I 也是一种 GSK-3 抑制剂。
    Bisindolylmaleimide I
  • HY-16294
    LY2090314 Inhibitor 99.85%
    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。
    LY2090314
  • HY-10182A
    Laduviglusib monohydrochloride Inhibitor 99.93%
    Laduviglusib (CHIR-99021) monohydrochloride 是一种有效的选择性 GSK-3α/β 抑制剂，IC50 为 10 nM 和 6.7 nM。Laduviglusib monohydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib monohydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。Laduviglusib monohydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib monohydrochloride 能诱导细胞自噬 (autophagy)。
    Laduviglusib monohydrochloride
  • HY-10182R
    Laduviglusib (Standard) Inhibitor
    Laduviglusib (Standard) 是 Laduviglusib 的标准品。Laduviglusib (CHIR-99021) 是一种有效的，选择性的，具有口服活性的 GSK-3α/β 抑制剂，IC50 为 10 nM 和 6.7 nM。Laduviglusib 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib 能诱导细胞自噬 (autophagy)。
    Laduviglusib (Standard)
  • HY-112388
    GSK-3b Inhibitor XI Inhibitor 99.10%
    GSK-3b Inhibitor XI 是糖原合酶激酶 3β (GSK3β；Ki=25 nM) 的强效抑制剂。浓度为 10 μM 时，该抑制剂对 79 种激酶中的 GSK3β 具有选择性。GSK-3b Inhibitor XI 可抑制 HEK293 细胞中的 GSK3β (EC50=32 nM)。
    GSK-3b Inhibitor XI
  • HY-162638
    GSK-3β inhibitor 18 Inhibitor
    GSK-3β inhibitor 18 (compound 2) 是 GSK-3β 的有效抑制剂，IC50 为 0.0021 μM。
    GSK-3β inhibitor 18
  • HY-12302
    Kenpaullone

    肯帕罗酮

    		Inhibitor 98.20%
    Kenpaullone 是一种有效的 CDK1/cyclin B 和 GSK-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。Kenpaullone，一种 KLF4 的小分子抑制剂，在体外降低乳腺癌干细胞的自我更新和细胞活力。
    Kenpaullone
  • HY-10590
    TWS119 Inhibitor 99.20%
    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。
    TWS119
  • HY-10580
    GSK 3 Inhibitor IX Inhibitor 99.74%
    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/β 和 CDK1-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。
    GSK 3 Inhibitor IX
  • HY-10182B
    Laduviglusib trihydrochloride Inhibitor 99.35%
    Laduviglusib (CHIR-99021) trihydrochloride 是一种有效的选择性 GSK-3α/β 抑制剂，IC50 为 10 nM 和 6.7 nM。CHIR-99021 trihydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。Laduviglusib trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib trihydrochloride 能诱导细胞自噬 (autophagy)。
    Laduviglusib trihydrochloride
  • HY-14872
    Tideglusib Inhibitor 99.79%
    Tideglusib (NP031112) 是一种不可逆的 GSK-3 抑制剂，抑制 GSK-3βWT 和GSK-3βC199A 的 IC50 分别为5 nM，60 nM。
    Tideglusib
  • HY-B0712B
    Ceftriaxone sodium salt

    头孢曲松钠盐

    		Inhibitor 99.25%
    Ceftriaxone sodium salt (Ro 13-9904) 是一种广谱 β-内酰胺类三代头孢菌素类抗生素 (antibiotic)，对多种革兰氏阴性菌和阳性菌有良好的抗菌活性。Ceftriaxone sodium salt 是 GSK3β 的共价抑制剂，IC50 值为 0.78 μM。Ceftriaxone sodium salt 是 Aurora B 的抑制剂。Ceftriaxone sodium salt 具有抗炎、抗肿瘤和抗氧化活性。Ceftriaxone sodium salt 可用于治疗细菌性感染和脑膜炎的研究。
    Ceftriaxone sodium salt
  • HY-10512
    AR-A014418 Inhibitor 99.14%
    AR-A014418 是一种有效，选择性，ATP 竞争性的 GSK3β 抑制剂 (IC50=104 nM; Ki=38 nM)。
    AR-A014418
  • HY-124719
    hSMG-1 inhibitor 11j Inhibitor 99.82%
    hSMG-1 inhibitor 11j，一种嘧啶衍生物，是有效的和选择性的 hSMG-1 抑制剂，IC50 值为 0.11 nM。hSMG-1 inhibitor 11j 对 hSMG-1 的选择性是 mTOR (IC50=50 nM)，PI3Kα/γ (IC50=92/60 nM) 和 CDK1/CDK2 (IC50=32/7.1 μM) 的 455 倍以上。hSMG-1 inhibitor 11j 可用于癌症研究。
    hSMG-1 inhibitor 11j
  • HY-B0320A
    Cromolyn sodium

    色甘酸钠

    		Inhibitor 99.93%
    Cromolyn sodium (Disodium Cromoglycate; FPL-670) 是抗过敏化合物。Cromolyn sodium 是一种 GSK-3β 抑制剂，IC50 为 2.0 μM。
    Cromolyn sodium
  • HY-137894A
    Tagtociclib hydrate Inhibitor 99.95%
    PF-07104091 hydrate 是一种高效选择性的 CDK2/cyclin E1 和 GSK3β 抑制剂，其 Ki 分别为 1.16 和 537.81 nM。PF-07104091 hydrate 对细胞周期素扩增的癌症具有抗肿瘤活性，来自专利 WO2020157652A2。
    Tagtociclib hydrate
  • HY-12292
    IM-12 Inhibitor 99.61%
    IM-12 是 GSK-3β 的抑制剂，IC50 值为 53 nM，可增强 Wnt 信号传导。
    IM-12
  • HY-113914
    9-ING-41 Inhibitor 99.13%
    9-ING-41 (Elraglusib) 是一种基于马来酰亚胺的 ATP 竞争性和选择性的糖原合酶激酶-3β (GSK-3β) 抑制剂，IC50 为 0.71 μM。9-ING-41 显著导致癌细胞的细胞周期停滞，自噬和凋亡。9-ING-41 具有抗癌活性，并具有增强化疗活性分子抗肿瘤作用的潜力。
    9-ING-41
目录号 产品名 / 同用名 种属 表达系统
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Download GSK-3 Signaling Pathway Map.

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. 

GSK-3 Isoform Comparison

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