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Submit ReviewKenpaullone is a GSK-3beta inhibitor (IC50 = 0.23 μM). Also inhibits cyclin dependent kinases (cdks) in the sub micromolar range (reported IC50 values are 0.4, 0.68-7 and 0.85 μM for cdk1, cdk2 and cdk5, respectively). Generates induced pluripotent stem cells (iPSCs) from somatic cells when used in combination with reprogramming factors; can replace Klf4.
Kenpaullone is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 327.18 |
公式 | C16H11BrN2O |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 142273-20-9 |
PubChem ID | 3820 |
InChI Key | QQUXFYAWXPMDOE-UHFFFAOYSA-N |
Smiles | BrC1=CC=C2NC3=C(CC(=O)NC4=CC=CC=C34)C2=C1 |
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 | 32.72 | 100 |
以下数据基于产品分子量 327.18。 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 |
---|---|---|---|
1 mM | 3.06 mL | 15.28 mL | 30.56 mL |
5 mM | 0.61 mL | 3.06 mL | 6.11 mL |
10 mM | 0.31 mL | 1.53 mL | 3.06 mL |
50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
参考文献是支持产品生物活性的出版物。
Buolamwini (2000) Cell cycle targets in novel anticancer drug discovery. Curr.Pharm.Des. 6 379 PMID: 10788588
Schultz et al (1999) Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J.Med.Chem. 42 2909 PMID: 10425100
Zaharevitz et al (1999) Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 59 2566 PMID: 10363974
Lyssiotis et al (2009) Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc.Natl.Acad.Sci.U.S.A. 106 8912 PMID: 19447925
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 Kenpaullone, please let us know.
关键词: Kenpaullone, Kenpaullone supplier, GSK-3β, GSK-3beta, inhibitors, inhibits, cdks, Potent, cyclin-dependent, kinase, GSK, Glycogen, Synthase, Kinase, 3, beta, Kinases, Cdk, Cyclin-Dependent, Protein, Carbohydrate, Metabolism, CDK1/cyclin, B, CDK2/cyclin, A, E, CDK5/cyclin/p35, stem, cells, Cyclin-dependent, Stem, Cell, Reprogramming, Non-selective, CDKs, 1398, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Kenpaullone 的部分引用包括:
Du et al (2015) Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells. Nat Commun 6 6626 PMID: 25806427
Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004
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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.