SB 415286
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SB415286是糖原合酶激酶-3(GSK-3)强效选择性的细胞渗透性抑制剂,Ki值为31 nM,对GSK-3和GSK3β效力相当[1]。
在人肝细胞中,SB415286抑制GSK3的活性,促进糖原合成,在HEK293细胞中,SB415286诱导连环蛋白-LEF / TCF调节的报告基因的表达[1]。在原代神经元中,它可以阻止PI3K途径诱导的细胞死亡[2]。进一步研究发现,SB415286降低GSK3β的活性,抑制雷帕霉素(rapamycin)介导的细胞周期蛋白D1下调、细胞周期停滞和化学敏感性[3]。GSK-3β的药物抑制大幅度损伤了p53依赖性的p21和Puma的转录激活,易化了p53依赖性的Bax的构象激活,最终导致p53介导的损伤应答从细胞周期停滞转化为细胞凋亡[4]。SB-415286通过线粒体相关机制减少缺血再灌注损伤。SB-415286减少腺嘌呤核苷酸转运和VDAC的磷酸化,增加Bcl-2与线粒体结合,阻止心肌中线粒体通透性转换孔开放[5]。在辐射诱导的细胞凋亡中,SB-415286对海马神经元产生保护作用。SB-415286抑制GSK-3β,可能会导致MDM2的上调,反过来调节p53的降解和p53依赖性细胞反应[6]。
在小鼠模型进一步证实,SB415286对辐射诱导的中枢神经系统坏死具有神经保护作用。在辐射前用SB415286处理小鼠,即靶向左半球的单个45-Gy部分,通过在体MRI进行检测,与DMSO处理的小鼠相比,SB415286对辐射诱导的坏死具有显著的的保护作用[7]。
参考文献:
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803.
Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J Neurochem. 2001 Apr;77(1):94-102.
Role of glycogen synthase kinase 3beta in rapamycin-mediated cell cycle regulation and chemosensitivity. Cancer Res. 2005 Mar 1;65(5):1961-72.
Pharmacologic modulation of glycogen synthase kinase-3beta promotes p53-dependent apoptosis through a direct Bax-mediated mitochondrial pathway in colorectal cancer cells. Cancer Res. 2005 Oct 1;65(19):9012-20.
Glycogen synthase kinase 3 inhibition slows mitochondrial adenine nucleotide transport and regulates voltage-dependent anion channel phosphorylation. Circ Res. 2008 Oct 24;103(9):983-91. doi: 10.1161/CIRCRESAHA.108.178970. Epub 2008 Sep 18.
Glycogen synthase kinase 3β inhibitors protect hippocampal neurons from radiation-induced apoptosis by regulating MDM2-p53 pathway. Cell Death Differ. 2012 Mar;19(3):387-96. doi: 10.1038/cdd.2011.94. Epub 2011 Jul 8.
A GSK-3β inhibitor protects against radiation necrosis in mouse brain. Int J Radiat Oncol Biol Phys. 2014 Jul 15;89(4):714-21. doi: 10.1016/j.ijrobp.2014.04.018.
Physical Appearance | A solid |
Storage | Store at RT |
M.Wt | 359.73 |
Cas No. | 264218-23-7 |
Formula | C16H10ClN3O5 |
Solubility | insoluble in H2O; ≥18 mg/mL in DMSO; ≥44.9 mg/mL in EtOH with ultrasonic |
Chemical Name | 3-(3-chloro-4-hydroxyanilino)-4-(2-nitrophenyl)pyrrole-2,5-dione |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C(=C1)C2=C(C(=O)NC2=O)NC3=CC(=C(C=C3)O)Cl)[N+](=O)[O-] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | SB415286是一种强效的GSK3α抑制剂,IC50和Ki值分别为78 nM和31 nM。 | |||||
靶点 | GSK-3α | GSK-3β | ||||
IC50 | 78 nM (Ki=31 nM) | ~78 nM |
质量控制和MSDS
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