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 (CT99021) 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 对 GSK-3 的选择性比 CDC2,ERK2 和其他蛋白激酶高 500 倍以上。CHIR-99021 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。CHIR-99021 能诱导细胞自噬 (autophagy)。
  • HY-12012
    SB 216763 Inhibitor 99.30%
    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-11012
    TDZD-8 Inhibitor 99.76%
    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-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 99.49%
    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-P1113
    Phospho-Glycogen Synthase Peptide-2(substrate)
    Phospho-Glycogen Synthase Peptide-2 (substrate) 是糖原合酶激酶-3 (GSK-3) 的肽底物,可用于蛋白丝氨酸激酶的亲和纯化。
  • HY-P1113A
    Phospho-Glycogen Synthase Peptide-2(substrate) TFA
    Phospho-Glycogen Synthase Peptide-2 (substrate) 是糖原合酶激酶-3 (GSK-3) 的肽底物,可用于蛋白丝氨酸激酶的亲和纯化。
  • HY-P1114A
    2B-(SP) (TFA)
    2B-(SP) TFA 是基于 eIF2B 的糖原合成酶激酶-3 (GSK-3) 底物。2B-(SP) TFA 容易被 GSK-3α 的 GSK-3β 磷酸化。
  • HY-10182A
    CHIR-99021 monohydrochloride Inhibitor 99.93%
    CHIR-99021 monohydrochloride (CT99021 monohydrochloride) 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 monohydrochloride 对 GSK-3 的选择性比 CDC2,ERK2 和其他蛋白激酶高 500 倍以上。CHIR-99021 monohydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 monohydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。CHIR-99021 monohydrochloride 能诱导细胞自噬 (autophagy)。
  • HY-B0320A
    Cromolyn sodium Inhibitor 99.10%
    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。
  • HY-12302
    Kenpaullone Inhibitor
    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。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。
  • HY-10182B
    CHIR-99021 trihydrochloride Inhibitor 98.01%
    CHIR-99021 trihydrochloride (CT99021 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。CHIR-99021 trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。CHIR-99021 trihydrochloride 能诱导细胞自噬 (autophagy)。
  • HY-10014
    R547 Inhibitor 99.66%
    R547 是一种高效、选择性的,口服有效的 ATP 竞争性的 CDK 抑制剂,对 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的 Ki 值分别为 2 nM、3 nM、1 nM。
  • 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-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-12292
    IM-12 Inhibitor 98.30%
    IM-12 是 GSK-3β 的抑制剂,IC50 值为 53 nM,可增强 Wnt 信号传导。
  • HY-15438
    SB 415286 Inhibitor 99.72%
    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-15356
    BIO-acetoxime Inhibitor >98.0%
    BIO-acetoxime (BIA) 是一种有效、选择性的 GSK-3 抑制剂,对 GSK-3α/β 的 IC50 值均为 10 nM;BIO-acetoxime 具有抗惊厥和抗感染作用。
  • HY-12524
    Bikinin Inhibitor 99.94%
    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-100207
    CP21R7 Inhibitor 99.77%
    CP21R7 是一种有效的 GSK-3β 抑制剂,IC50 值为 1.8 nM;CP21R7 同时可抑制 PKCαIC50 值为 1900 nM。

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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