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Submit ReviewBIO is a potent ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 = 5 nM). Also inhibits cyclin-dependent kinases (cdks; IC50 values are <100 nM for cdk2 and 5 and sub micromolar for cdk1, cdk4 and cdk9). Maintains self-renewal and pluripotency in embryonic stem cells via activation of the Wnt signaling pathway in vitro; also promotes proliferation and dedifferentiation in cardiomyocytes.
Negative Control also available.
分子量 | 356.17 |
公式 | C16H10BrN3O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 667463-62-9 |
PubChem ID | 5287844 |
InChI Key | WNWSUJQVZJJGLF-SQFISAMPSA-N |
Smiles | O/N=C(C1=CC=CC=C1N2)/C2=C3/C(NC4=C3C=CC(Br)=C4)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 3.56 | 10 | |
ethanol | 3.56 | 10 |
以下数据基于产品分子量 356.17。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 28.08 mL | 140.38 mL | 280.76 mL |
0.5 mM | 5.62 mL | 28.08 mL | 56.15 mL |
1 mM | 2.81 mL | 14.04 mL | 28.08 mL |
5 mM | 0.56 mL | 2.81 mL | 5.62 mL |
参考文献是支持产品生物活性的出版物。
Meijer et al (2003) GSK-3-selective inhibitors derived from tyrian purple indirubins. Chem.Biol. 10 1255 PMID: 14700633
Polychronopoulos et al (2004) Structural basis for the synthesis of indirubins as potent and selective inhibtors of glycogen synthase kinase-3 and cyclin dependent kinases. J.Med.Chem. 47 935 PMID: 14761195
Tseng et al (2006) The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem.Biol. 13 957 PMID: 16984885
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
If you know of a relevant reference for BIO, please let us know.
关键词: BIO, BIO supplier, Potent, selective, GSK-3, inhibitors, inhibits, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, stem, cells, hematopoietic, haematopoietic, HSC, 6BIO, Kinase, Stem, Cell, Proliferation, Signaling, Non-selective, CDKs, Hematopoietic, Cells, 3194, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BIO 的部分引用包括:
Roy et al (2017) Myotome adaptability confers developmental robustness to somitic myogenesis in response to fibre number alteration. Dev Biol 431 321 PMID: 28887016
Zhang et al (2015) GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis. PLoS Biol 13 e1002129 PMID: 25860027
Berger et al (2014) PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis. Cell Cycle 28 629 PMID: 24263804
Lu et al (2014) Tissue-specific derepression of TCF/LEF controls the activity of the Wnt/β-catenin pathway. Sci Rep 5 5368 PMID: 25371059
Fleskens et al (2019) Nemo-like Kinase Drives Foxp3 Stability and Is Critical for Maintenance of Immune Tolerance by Regulatory T Cells. Cell Rep 26 3600 PMID: 30917315
Stevens et al (2017) Genomic integration of Wnt/β-catenin and BMP/Smad1 signaling coordinates foregut and hindgut transcriptional programs. Development 144 1283 PMID: 28219948
Diamantopoulou et al (2017) TIAM1 Antagonizes TAZ/YAP Both in the Destruction Complex in the Cytoplasm and in the Nucleus to Inhibit Invasion of Intestinal Epithelial Cells. Cancer Cell 31 621 PMID: 28416184
Duffy et al (2016) Wnt signalling is a bi-directional vulnerability of cancer cells. Oncotarget 7 60310 PMID: 27531891
Naujok et al (2014) Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors. BMC Res Notes 7 273 PMID: 24779365
Guo et al (2012) Slug and Sox9 cooperatively determine the mammary stem cell state. World J Gastroenterol 148 1015 PMID: 22385965
Penas et al (2015) GSK3 inhibitors stabilize Wee1 and reduce cerebellar granule cell progenitor proliferation. Nat Commun 14 417 PMID: 25616418
Rhim et al (2015) A High-content screen identifies compounds promoting the neuronal differentiation and the midbrain DA neuron specification of human neural progenitor cells. Elife 5 16237 PMID: 26542303
Lindström et al (2015) Integrated β-catenin, BMP, PTEN, and Notch signalling patterns the nephron. Nat Chem Biol 3 e04000 PMID: 25647637
Thorne et al (2015) GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. Stem Cells Transl Med 11 58 PMID: 25402767
Efthymiou et al (2015) Rescue of an in vitro neuron phenotype identified in Niemann-Pick disease, type C1 induced pluripotent stem cell-derived neurons by modulating the WNT pathway and calcium signaling. Elife 4 230 PMID: 25637190
Pronobis et al (2015) A novel GSK3-regulated APC:Axin interaction regulates Wnt signaling by driving a catalytic cycle of efficient βcatenin destruction. Cell 4 e08022 PMID: 26393419
Duffy et al (2014) GSK3 inhibitors regulate MYCN mRNA levels and reduce neuroblastoma cell viability through multiple mechanisms, including p53 and Wnt signaling. Mol Cancer Ther 13 454 PMID: 24282277
Volpini et al (2018) Trypanosoma cruzi Exploits Wnt Signaling Pathway to Promote Its Intracellular Replication in Macrophages. Front Immunol 9 859 PMID: 29743880
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.