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-144290
    ARN25068 Inhibitor 99.66%
    ARN25068 是三种蛋白激酶 GSK-3β、FYN 和 DYRK1A的亚微摩尔抑制剂，可解决 tau 蛋白过度磷酸化。
    ARN25068
  • HY-126144A
    (E/Z)-GSK-3β inhibitor 1 Inhibitor 99.03%
    (E/Z)-GSK-3β inhibitor 1 是 (E)-GSK-3β inhibitor 1 和 (Z)-GSK-3β inhibitor 1 的消旋体。GSK-3β inhibitor 1 (compound 3a) 是糖原合成酶激酶 3β (GSK-3β)的抑制剂，可用于糖尿病的研究，其对 GSK-3β 的 IC50 值为 4.9 nM。
    (E/Z)-GSK-3β inhibitor 1
  • HY-117822
    BRD0209 Inhibitor 99.56%
    BRD0209 是一种有效、选择性和双重的 GSK3α/β 抑制剂 (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM)。BRD0209 还是一种可逆的 ATP 竞争性抑制剂，具有快关动力学 (Ki 分别为 4.2 nM)。BRD0209 是一种三环吡唑并四氢喹啉酮化合物。BRD0209 具有研究心境障碍疾病的潜力。
    BRD0209
  • HY-134393B
    6-Me-ATP trisodium Chemical ≥99.0%
    6-Me-ATP (N6-Methyl-ATP) trisodium 是一种 N6 修饰的 ATP 衍生物。6-Me-ATP trisodium 对 GSK3 显示出很好的结合亲和力，可作为 GSK3β 催化其底物肽磷酸化的磷酸基团供体。
    6-Me-ATP trisodium
  • HY-121035
    7BIO Inhibitor ≥98.0%
    7BIO (7-Bromoindirubin-3-Oxime) 是靛玉红的衍生物。7BIO (7-Bromoindirubin-3-Oxime) 对细胞周期蛋白依赖性激酶5 (CDK5) 和糖原合酶激酶-3β (GSK3β) 具有抑制作用。7BIO (7-Bromoindirubin-3-Oxime) 抑制 Aβ 寡聚体诱导的神经炎症、突触损伤、tau 过度磷酸化、星形胶质细胞和小胶质细胞的活化，并减轻 Aβ 寡聚体诱导的小鼠认知障碍[1]。
    7BIO
  • HY-15504A
    RGB-286638 free base Inhibitor 98.87%
    RGB-286638 是一种有效的 CDK 抑制剂，抑制 cyclin T1-CDK9，cyclin B1-CDK1，cyclin E-CDK2，cyclin D1-CDK4，cyclin E-CDK3 和 p35-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。
    RGB-286638 free base
  • HY-139254
    Indirubin-3′-oxime Inhibitor 99.49%
    Indirubin-3′-oxime (IDR3O) 是 indirubin 的合成衍生物，是细胞周期蛋白依赖性激酶 (CDKs) 和糖原合成酶激酶3β (GSK3β) 的有效抑制剂。Indirubin-3′-oxime 直接抑制JNK的所有三种亚型 (JNK1，JNK2，JNK3) 的活性，IC50s 分别为 0.8 μM、1.4 μM 和 1 μM。Indirubin-3′-oxime 可通过激活软骨细胞中的 Wnt/β-catenin 信号来促进身高增长。
    Indirubin-3′-oxime
  • HY-13867A
    Bisindolylmaleimide I hydrochloride

    3-[1-[3-(二甲基氨基)丙基]-1H-吲哚-3-基]-4-(1H-吲哚-3-基)-1H-吡咯-2,5-二酮单盐酸盐

    		99.18%
    Bisindolylmaleimide I (GF109203X) hydrochloride 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 hydrochloride 也是一种 GSK-3 抑制剂。
    Bisindolylmaleimide I hydrochloride
  • HY-141480
    GSK-3β inhibitor 3 Inhibitor 98.20%
    GSK-3β inhibitor 3 是一种有效，选择性，不可逆和共价的糖原合酶激酶 3β (GSK-3β) 抑制剂，IC50 值为 6.6 μM。GSK-3β inhibitor 3 可用于急性早幼粒细胞白血病的研究。
    GSK-3β inhibitor 3
  • HY-122665A
    HTH-01-091 TFA Inhibitor 99.48%
    HTH-01-091 TFA 是一种强效且选择性的 maternal embryonic leucine zipper kinase (MELK) 抑制剂，其 IC50 为 10.5 nM。HTH-01-091 TFA 还能抑制 PIM1/2/3、RIPK2、DYRK3、smMLCK 和 CLK2。HTH-01-091 TFA 可用于乳腺癌研究。
    HTH-01-091 TFA
  • HY-107815
    CHIR 98024 Inhibitor 98.08%
    CHIR 98024 (Compound L) 是一种糖原合成酶激酶 3 （GSK3）抑制剂，EC50 为 0.2566 μM。
    CHIR 98024
  • HY-14679
    GSK3β inhibitor II Inhibitor 99.76%
    GSK3β inhibitor II 是 GSK3β 的抑制剂。GSK3β inhibitor II 可用于阿尔茨海默病 (AD) 的研究。
    GSK3β inhibitor II
  • HY-122665
    HTH-01-091 Inhibitor 98.64%
    HTH-01-091 是一种强效且选择性的 maternal embryonic leucine zipper kinase (MELK) 抑制剂，其 IC50 为 10.5 nM。HTH-01-091 还能抑制 PIM1/2/3、RIPK2、DYRK3、smMLCK 和 CLK2。HTH-01-091 可用于乳腺癌研究。
    HTH-01-091
  • HY-P4858
    C-Peptide 1 (rat) Activator 99.80%
    C-Peptide 1 (rat) 是一种肽，是 β-catenin/GSK-3β 激活剂。C-Peptide 1 (rat) 可调节 Wnt/β-catenin 信号通路。C-Peptide 1 (rat) 可用于癌症研究。
    C-Peptide 1 (rat)
  • HY-111055
    BIP-135 Inhibitor 99.86%
    BIP-135 是一个高效、选择性的，ATP 竞争性的 GSK-3 抑制剂，对 GSK-3α 和 GSK-3β 作用的IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。
    BIP-135
  • HY-P1113A
    Phospho-Glycogen Synthase Peptide-2(substrate) TFA 98.02%
    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。
    Phospho-Glycogen Synthase Peptide-2(substrate) TFA
  • HY-134622
    GSK-3/CDK5/CDK2-IN-1 Inhibitor 98.10%
    GSK-3/CDK5/CDK2-IN-1，一种咪唑衍生物，是 cdk5，cdk2 和 GSK-3 的抑制剂。GSK-3/CDK5/CDK2-IN-1 可用于癌症和神经退行性疾病的研究。详细信息请参考专利文献 WO2002010141A1 中的化合物 9a。
    GSK-3/CDK5/CDK2-IN-1
  • HY-111930
    5-Iodo-indirubin-3'-monoxime Inhibitor 99.50%
    5-Iodo-indirubin-3'-monoxime 是一种有效的 GSK-3β，CDK5/P25 和 CDK1/cyclin B 抑制剂，与 ATP 竞争性地结合酶的催化位点，IC50 值分别为 9，20 和 25 nM。
    5-Iodo-indirubin-3'-monoxime
  • HY-P2558
    GSK3 Substrate, α, β subunit 99.83%
    GSK3 Substrate, α, β subunit 是糖原合酶激酶-3 (GSK-3) 的肽底物，可用于测量 GSK-3 活性。
    GSK3 Substrate, α, β subunit
  • HY-40294
    Indazole Inhibitor 99.72%
    吲哚唑，又称异吲哚唑 (isoindazole)，是一种杂环芳香有机化合物。其衍生物表现出广泛的生物活性，包括抗炎、抗菌、抗艾滋病、抗心律失常、抗真菌和抗肿瘤的特性。吲哚唑及其衍生物可用于癌症、神经系统疾病、心血管疾病、胃肠道疾病的研究。
    Indazole
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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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