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AdipoGen Life Sciences
(R)-Roscovitine
230
CHF
CHF 230.00
In stock
AG-MR-C0001-M02525 mgCHF 230.00
| Product Details | |
|---|---|
| Synonyms | Seliciclib; CYC201; 6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H26N6O |
| MW | 354.5 |
| CAS | 186692-46-6 |
| Purity Chemicals | ≥99% (NMR) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO or ethanol. Slightly soluble in water. |
| Reconstitution | Stock solutions can be made up to 10mM in DMSO. |
| Identity | Determined by 1H-NMR. |
| InChi Key | BTIHMVBBUGXLCJ-OAHLLOKOSA-N |
| Smiles | CC[C@H](CO)NC1=NC2=C(N=CN2C(C)C)C(NCC2=CC=CC=C2)=N1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice |
After reconstitution, prepare aliquots and store at -20°C. Protect from light and moisture. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent and selective inhibitor of cyclin dependent kinases CDK1, CDK2, CDK5, CDK7 and CDK9.
- Pyridoxal kinase (PDXK) inhibitor.
- Triggers cell apoptotic cell death.
- Down-regulates Mcl-1 and MYCN.
- Anticancer compound. Kills chronic lymphocytic leukemia (LLC) cells and slows tumor growth in mouse xenografts.
- Inhibits cysts formation in culture and in polycystic kidney disease (PKD) mouse models.
- Potential anti-inflammatory compound that can influence the resolution of inflammation.
- Potential antidiabetic compound. Shown to protect pancreatic β-cells from glucotoxicity and increase insulin secretion.
- Shows antiviral properties.
- Neuroprotective in brain trauma.
- Has positive effects on Timothy syndrome cells.
- Used for cloning of mammals by synchronization of nucleus donor cells.
- Provides neuroprotection in experimental traumatic brain injury.
Product References
- Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5: L. Meijer, et al.; Eur. J. Biochem. 243, 527 (1997)
- Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997)
- Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine: WF. De Azevedo, et al.; Eur. J. Biochem. 243, 518 (1997)
- Pharmacological cyclin-dependent kinase inhibitors inhibit replication of wild-type and drug-resistant strains of Herpes simplex virus and Human immunodeficiency virus type 1 by targeting cellular, not viral, proteins: L.M. Schang, et al.; J. Virol. 76, 7874 (2002)
- Enhanced survivability of cloned calves derived from roscovitine-treated adult somatic cells: J. Gibbons, et al.; Biol. Reprod. 66, 895 (2002)
- Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials: L. Meijer & E. Raimond; Acc. Chem. Res. 36, 417 (2003)
- Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives: L. Tang, et al.; J. Biol. Chem. 280, 31220 (2005)
- Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005)
- Inhibition of cyclin-dependent kinase 5 activity protects pancreatic beta cells from glucotoxicity: M. Ubeda, et al.; J. Biol. Chem. 281, 28858 (2006)
- Cyclin-dependent kinase inhibitors enhance the resolution of inflammation by promoting inflammatory cell apoptosis: A.G. Rossi, et al.; Nature Med. 12, 1056 (2006)
- Long-lasting arrest of murine polycystic kidney disease with CDK inhibitor Roscovitine: N.O. Bukanov, et al.; Nature 444, 949 (2006)
- Production of cloned horse foals using roscovitine-treated donor cells and activation with sperm extract and/or ionomycin: K. Hinrichs, et al.; Reproduction 134, 319 (2007)
- CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases: K. Bettayeb, et al.; Oncogene 27, 5797 (2008)
- Practical Synthesis of Roscovitine and CR8: N. Oumata, et al.; Org. Process Res. Dev. 13, 641 (2009)
- CDK inhibitors Roscovitine and CR8 trigger Mcl-1 down-regulation and apoptotic cell death in neuroblastoma cells: K. Bettayeb, et al.; Genes & Cancer 1, 369 (2010)
- Using induced pluripotent stem cells to investigate cardiac phenotypes in Timothy syndrome: M. Yazawa; Nature 471, 230 (2011)
- CDK inhibitors R-roscovitine and S-CR8 effectively block renal and hepatic cystogenesis in an orthologous model of ADPKD: N.O. Bukanov, et al.; Cell Cycle 11, 4040 (2012)
- Selective CDK inhibitor limits neuroinflammation and progressive neurodegeneration after brain trauma: S.V. Kabadi, et al.; J. Cereb. Blood Flow Metab. 32, 137 (2012)
- Roscovitine is a proteostasis regulator that corrects the trafficking defect of F508del-CFTR by a CDK-independent mechanism: C. Norez, et al.; Br. J. Pharmacol. 171, 4831 (2014)
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