GSK-3 (糖原合成酶激酶3)

Glycogen synthase kinase-3; Glycogen synthase kinase 3

糖原合酶激酶 3 (GSK-3) 是一种多功能丝氨酸/苏氨酸激酶，由两种亚型组成，即 α 和 β。它是受体酪氨酸激酶、细胞因子和 Wnt 信号通路的高度保守负调节剂。这些通路的刺激会抑制 GSK-3 调节各种下游效应因子，包括转录因子、营养传感器、糖原合成、线粒体功能、昼夜节律和细胞命运。GSK-3 还调节响应 T 细胞受体激活的选择性剪接，最近的磷酸化蛋白质组学研究表明，多种剪接因子和 RNA 生物合成调节因子以 GSK-3 依赖的方式进行磷酸化。

GSK-3 的功能障碍或异常活动会导致多种疾病，如阿尔茨海默病 (AD) 和其他神经退行性疾病，以及其他类型的疾病，如糖尿病、心血管疾病和癌症。GSK-3 还与针对病原体的先天免疫反应有关，这使得 GSK-3 成为治疗干预的绝佳靶点。

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

GSK-3 相关产品 (240)
重组蛋白 (4)
抗体 (9)
GSK-3 信号通路
GSK-3 Isoform Comparison

By Effects:	抑制剂 (199) 降解剂 (2) 激活剂 (17) 调节剂 (2) 化学品 (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-B0712A

Ceftriaxone sodium hydrate 头孢曲松钠水合物	Inhibitor	99.25%
Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) 是一种广谱 β-内酰胺类三代头孢菌素类抗生素，对多种革兰氏阴性菌和阳性菌有良好的抗菌活性。Ceftriaxone sodium hydrate 是 GSK3β 的共价抑制剂，IC₅₀ 值为 0.78 μM。 Ceftriaxone sodium hydrate 是 Aurora B 的抑制剂。Ceftriaxone sodium hydrate 具有抗炎、抗肿瘤和抗氧化活性。Ceftriaxone sodium hydrate 可用于治疗细菌性感染和脑膜炎的研究。

HY-112809

GSK2646264	Inhibitor	98.39%
GSK2646264 (Compound 44) 是一种有效的、选择性的脾酪氨酸激酶 (SYK) 抑制剂，pIC₅₀ 值为 7.1。GSK2646264 对其他激酶也有抑制效果，对 LCK、LRRK2、GSK3β、JAK2、VEGFR2、Aurora B 和 Aurora A 的 pIC₅₀ 分别为 5.4、5.4、5.3、5、4.5、<4.6 和 <4.3。GSK2646264 可渗透到皮肤的表皮和真皮层。

HY-13973A

GSK-3 inhibitor 1	Inhibitor	99.89%
GSK-3 inhibitor 1 (化合物 core 3) 是一种 GSK-3 抑制剂。GSK-3 inhibitor 1 能诱导干细胞/祖细胞自我更新 (如诱导干/祖细胞增殖，同时在子代细胞中维持分化成组织细胞的能力)。

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。

HY-117025A

Manzamine A hydrochloride	Inhibitor	99.66%
Manzamine A hydrochloride 是一种具有口服活性的 β-carboline 生物碱，抑制 GSK-3β 和 CDK-5 的 IC₅₀ 值为 10.2 μM 和 1.5 μM。Manzamine A hydrochloride 靶向胰腺癌细胞的 vacuolar ATPases 并抑制自噬 (autophagy)。Manzamine A hydrochloride 具有抗疟和抗癌活性。Manzamine A hydrochloride 对 HSV-1 具有较强的活性。

HY-149845

PROTAC GSK-3β Degrader-1	Degrader	99.05%
PROTAC GSK-3β Degrader-1 (compound 1) 是靶向 GSK-3β 的降解剂，IC₅₀ 为 833 nM。 PROTAC GSK-3β Degrader-1 包含 SB-216763 (GSK-3β 抑制剂), PEG 连接子和 CRBN (E3 连接酶配体)。 PROTAC GSK-3β Degrader-1 降低 Aβ_25-35 肽和 CuSO₄ 诱导的神经毒性。PROTAC GSK-3β Degrader-1 可用于研究阿尔茨海默病。

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)。

HY-134393B

6-Me-ATP (trisodium) solution (100mM)	Chemical	99.89%
6-Me-ATP (N6-Methyl-ATP) trisodium solution (100mM) 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。

HY-141480

GSK-3β inhibitor 3	Inhibitor	99.22%
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。

HY-126144

GSK-3β inhibitor 1	Inhibitor	98.04%
GSK-3β inhibitor 1 (compound 3a) 抑制 GSK-3β，IC₅₀ 为 4.19 nM。 GSK-3β inhibitor 1 在 Streptozotocin (HY-13753) 处理的大鼠模型中显示出很高的抗糖尿病功效。

HY-153166

PT-65	Degrader	98.4%
PT-65 是一种有效的、选择性 GSK3 PROTAC 降解剂，对 SH-SY5Y 细胞中 GSK3α (DC₅₀= 28.3 nM) 和 GSK3β (DC₅₀ = 34.2 nM) 的降解能力最强。PT-65 可用于阿尔茨海默病的研究。(Pink: GSK3 inhibitor (HY-15761); Black: linker; Blue: CRBN Ligand (HY-10984))

HY-164907

GSK-3β inhibitor 22	Inhibitor	98.57%
GSK-3β inhibitor 22 (compound 20o) 是一种 GSK-3β 抑制剂，IC₅₀ 为 3.1 nM。GSK-3β inhibitor 22 具有研究阿尔茨海默病的潜力。

HY-N3181

Nodosin	Inhibitor	98.44%
Nodosin 是一种可以从 Isodon serra 中分离得到的具有口服活性的二萜类化合物。Nodosin 可抑制肿瘤细胞增殖，诱导细胞周期阻滞和凋亡 (apoptosis)。Nodosin 也能抑制氧化应激、炎症反应和铁死亡 (ferroptosis)。 Nodosin 具有抗炎和抗肿瘤的活性。

HY-112392

GSK-3 Inhibitor XIII	Inhibitor	98.79%
GSK-3 Inhibitor XIII 是一种有效的 ATP 竞争性 GSK-3 抑制剂，K_i 为 24 nM。

HY-W969907

GSK3-IN-7		99.35%
GSK3a-IN-38 是一种突破性的小分子，可有效抑制 GSK-3a 活性。

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。

HY-100950

ABC1183	Inhibitor	99.19%
ABC1183 是一种具有口服活性的选择性 GSK3 和 CDK9 双重抑制剂。ABC1183 作用于 GSK3β, GSK3α 和 CDK9/cyclin T1 的 IC₅₀ 值分别是 657 nM、327 nM、321 nM。ABC1183 具有抗炎作用，抗肿瘤活性。

HY-112388

GSK-3b Inhibitor XI	Inhibitor	99.10%
GSK-3b Inhibitor XI (Compound 33) 是一种强效且选择性的 GSK3β 抑制剂，其 K_i 值为 25 nM。GSK-3b Inhibitor XI 可提高 glycogen synthase (GS) 活性。GSK-3b Inhibitor XI 可用于 2 型糖尿病和阿尔茨海默病研究。

HY-121035

7BIO	Inhibitor	99.20%
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]。

HY-120902

GSK-3β inhibitor 8	Inhibitor	≥99.0%
GSK-3β inhibitor 8 是一种噻吩嘧啶衍生物，是有效和选择性的 GSK-3β 抑制剂 (IC₅₀=64 nM)。GSK-3β inhibitor 8 负调控 Wnt 信号通路，刺激 β 细胞增殖。

β-catenin β-catenin β-catenin β-catenin DKK GSK-3 Axin APC CK1 CK1/CK2 GSK-3 Dvl Wnt Wnt Wnt Proteasome Axin Dvl GSK-3 GSK-3 sFRP, WIF-1, Cerberus eIF2B β-TrCP Cadherin β-catenin LGS PYGO TCF/LEF CBP Tiki Insulin/IGF IGF1R Glycogen
Synthase Glycogen Gene
Transcription
Cyclin D1, c-Myc,
Axin2, Brachyury, etc. c-Jun CREB HSF1 C-EBPβ STAT3 NF-κB IRS PI3K PIP2 PIP3 PTEN PDK1 PI3K SOS Grb2 Gas1 SHC Akt Trk receptor NT D2R β-arrestin2 PP2A Akt MAP Kinases BAD BAX 5-HT receptor 5-HT_1A 5-HT₂ MAP1B Apoptosis

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

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4