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干细胞诱导
糖尿病 GSK-3
/ SB-216763

SB-216763 {[allProObj[0].p_purity_real_show]}

货号：A100785

SB-216763是一种高效、选择性和ATP竞争性的GSK-3抑制剂，对GSK-3α和GSK-3β的IC50均为34.3 nM。SB216763增强培养小鼠成肌细胞中静止储备细胞的胰岛素诱导分化，刺激培养大鼠神经球中的神经干细胞分化。SB216763还诱导培养的人类神经前体细胞 (NPCs)的神经分化，促进培养小鼠造血祖细胞 (HPCs)中树突状细胞的分化。

SB-216763 化学结构 CAS号：280744-09-4
SB-216763 化学结构
CAS号：280744-09-4
SB-216763 3D分子结构
CAS号：280744-09-4
SB-216763 化学结构 CAS号：280744-09-4
SB-216763 3D分子结构 CAS号：280744-09-4
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SB-216763 纯度/质量文件 产品仅供科研

货号：A100785 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 GSK-3 ↓ GSK-3α ↓ GSK-3β ↓ 其他靶点 纯度
AZD2858 +

GSK-3, IC50: 68 nM

 		99%
Bikinin ✔ 99%+
GSK 3 Inhibitor IX ++++

GSK-3, IC50: 5 nM

 		99%+
AZD1080 +++

GSK-3α, IC50: 6.9 nM

 		++

GSK-3β, IC50: 31 nM

 		99%+
BIO-acetoxime +++

GSK-3α, IC50: 10 nM

 		+++

GSK-3β, IC50: 10 nM

 		95%
SB-216763 ++

GSK-3α, IC50: 34.3 nM

 		++

GSK-3β, IC50: ~34.3 nM

 		98%
SB 415286 +

GSK-3α, IC50: 78 nM

 		+

GSK-3β, IC50: ~78 nM

 		99%+
CHIR-98014 ++++

GSK-3α, IC50: 0.65 nM

 		++++

GSK-3β, IC50: 0.58 nM

 		98%
LY2090314 ++++

GSK-3α, IC50: 1.5 nM

 		++++

GSK-3β, IC50: 0.9 nM

 		99%+
CHIR 99021 +++

GSK-3α, IC50: 10 nM

 		++++

GSK-3β, IC50: 6.7 nM

 		99%+
TDZD-8 +

GSK-3β, IC50: 2 μM

 		99%+
Indirubin +

GSK-3β, IC50: 0.6 μM

 		98%
IM-12 ++

GSK-3β, IC50: 53 nM

 		98%
TWS119 ++

GSK-3β, IC50: 30 nM

 		99%
1-Azakenpaullone +++

GSK-3β, IC50: 18 nM

 		99%+
AR-A014418 ++

GSK-3β, Ki: 38 nM

 		99%+
Tideglusib +

GSK-3β, IC50: 60 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SB-216763 生物活性

靶点

  • GSK-3α

    GSK-3α, IC50:34.3 nM

  • GSK-3β

    GSK-3β, IC50:~34.3 nM
描述 GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase, consisting of GSK-3 and subunit, which plays a key role in many different biological processes including tumorigenesis, cell survival, and developmental patterning. GSK-3 is constitutively active in non-stimulated cells and can negatively regulate canonical Wnt/-catenin signaling[2][3]. SB-216763 is a maleimide-derived GSK-3 inhibitor with IC50 value of 34nM for GSK-3K (measured by recombinant human GSK-3K). SB-216763 is equally effective at inhibiting GSK-3 and SB-216763<6uM can induce transcription of a-catenin-LEF/TCF regulated reporter gene dose-dependently in serum starved HEK293 for 16h [1]. Treatment with 5uM SB-216763 for 4h can increase levels of cytoplasmic-catenin, which is a target negatively regulated by GSK-3, in both serum-starved cerebellar granule neurons and HEK293 cells. SB-216763 (3-5uM) can confer a marked reduction in GSK-3-dependent tau phosphorylation at Ser202-phosphoepitopes in transfected HEK293 cells and endogenous tau protein in cerebellar granule neurons[4]. SB-216763 can cross the blood–brain barrier and enter the CNS in both rodents and nonhuman primates[5]. Co-infusion of SB-216763 corrected all responses to Aβ infusion except the induction of gliosis and behavioral deficits in the Morris water maze of rats [6].
作用机制 Mechanism: SB-216763 can inhibit GSK-3 in an ATP competitive manner. [1]

SB-216763 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Diabetes model Tail intravenous injection 600 µg/kg Every 2 days for 2 months Inhibition of GSK-3β activity completely prevented diabetes-induced glycogen synthase phosphorylation, HK II downregulation, PPARα upregulation, PGC-1 downregulation, and lipid accumulation in the heart of the wild-type diabetic mice. Diabetes. 2009 Jun;58(6):1391-402
Mice TMEM43 mutant mouse model Intraperitoneal injection 2.5 mg/kg Daily To study the effect of SB-216763 on cardiac function in TMEM43 mutant mice, results showed that SB-216763 improved cardiac function and reduced cardiomyocyte death. Circulation. 2019 Oct;140(14):1188-1204
Mice LRP6+/− mice Intraperitoneal injection 1 mg/kg 16 hours SB-216763 inhibited GSK-3β activity and reversed the increased Ca2+-induced depolarization in LRP6+/? mice mitochondria Stroke. 2013 Aug;44(8):2284-2291
Mice Df(16)A+/− mouse model Intraperitoneal injection 2 mg/kg Every other day, from P7 to P28 Developmental inhibition of Gsk3 rescues deficits in hippocampal-prefrontal connectivity, task-related neural activity, and spatial working memory behavior in Df(16)A+/? mice. Neuron. 2016 Mar 2;89(5):1100-9
Mice Wild-type C57BL/6 mice Intraperitoneal injection 1-10 mg/kg Single dose, 10 minutes prior to NOR task training To investigate the role of GSK3 in the NOR task, results showed that SB216763-treated mice exhibited impaired performance in the NOR task and recognition memory. J Biomed Sci. 2020 Jan 3;27(1):16
Mice Bilateral renal ischemia-reperfusion injury model Intraperitoneal injection 20 mg/kg Single dose, lasting 14 days GSK3 inhibition alleviated bilateral IR-induced renal fibrosis and renal function impairment. Exp Mol Med. 2017 Jun 23;49(6):e347
Mice Adult mice Intraperitoneal injection 2 mg/kg Every other day for 2 weeks SB-216763 treatment significantly increased the number of BrdU positive cells and rescued the reduction in BrdU positive cells caused by DISC1 knockdown Cell. 2009 Mar 20;136(6):1017-31

SB-216763 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
HEK293 cells Function assay Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2 μM 12941331
human 5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM SANGER
human A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM SANGER
human A2058 cell Growth inhibition assay Inhibition of human A2058 cell growth in a cell viability assay, IC50=13.469 μM SANGER

SB-216763 参考文献

[1]Coghlan MP, Culbert AA, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803.

[2]Martinez A, Castro A, et al. Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation. Med Res Rev. 2002 Jul;22(4):373-84.

[3]Domoto T, Pyko IV, et al. Glycogen synthase kinase-3β is a pivotal mediator of cancer invasion and resistance to therapy. Cancer Sci. 2016 Oct;107(10):1363-1372.

[4]Cross DA, Culbert AA, et al. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J Neurochem. 2001 Apr;77(1):94-102.

[5]Li L, Shao X, et al. Synthesis and Initial in Vivo Studies with [(11)C] SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3. ACS Med Chem Lett. 2015 Mar 10;6(5):548-52.

[6]Hu S, Begum AN, et al. GSK3 inhibitors show benefits in an Alzheimer's disease (AD) model of neurodegeneration but adve

SB-216763 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.47mL

2.69mL

1.35mL

26.94mL

5.39mL

2.69mL

SB-216763 技术信息

CAS号280744-09-4
分子式C19H12Cl2N2O2
分子量 371.22
SMILES Code O=C(C(C1=CC=C(Cl)C=C1Cl)=C2C3=CN(C)C4=C3C=CC=C4)NC2=O
MDL No. MFCD09753369
别名
运输蓝冰
InChI Key JCSGFHVFHSKIJH-UHFFFAOYSA-N
Pubchem ID 176158
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(282.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: SB-216763 | SB 216763 | Diabete | GSK-3 | AmBeed-信号通路专用抑制剂 | SB-216763 纯度/质量文件 | SB-216763 亚型比较 | SB-216763 生物活性 | SB-216763 细胞研究 | SB-216763 参考文献 | SB-216763 实验方案 | SB-216763 技术信息

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