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Submit ReviewRoscovitine is a cyclin-dependent kinase (cdk) inhibitor. Displays sub-micromolar inhibition of cdk1, cdk2, cdk5, cdk7 and cdk9 (reported IC50 values range from 0.16 - 0.28 μM for cdk5 to 0.8 μM for cdk7). Selective for cdks over a wide range of related kinases including ERK1 and ERK2. Arrests L1210 cells in G1 phase. Inhibits phosphorylation of vimentin in vivo. Antimitotic.
Roscovitine is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 354.45 |
公式 | C19H26N6O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 186692-46-6 |
PubChem ID | 160355 |
InChI Key | BTIHMVBBUGXLCJ-OAHLLOKOSA-N |
Smiles | OC[C@@H](CC)NC1=NC(N(C(C)C)C=N2)=C2C(NCC3=CC=CC=C3)=N1 |
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 | 35.44 | 100 | |
ethanol | 35.44 | 100 |
以下数据基于产品分子量 354.45。 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 | 2.82 mL | 14.11 mL | 28.21 mL |
5 mM | 0.56 mL | 2.82 mL | 5.64 mL |
10 mM | 0.28 mL | 1.41 mL | 2.82 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
De Azevedo et al (1997) Inhibition of cyclin-dependent kinases by purine analogues. Eur.J.Biochem. 243 518 PMID: 9030780
Meijer (1996) Chemical inhibitors of cyclin-dependent kinases. Trends Cell.Biol. 6 393 PMID: 15157522
Meijer et al (1997) Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur.J.Biochem. 243 527 PMID: 9030781
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 Roscovitine, please let us know.
关键词: Roscovitine, Roscovitine supplier, , Tocris Bioscience
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