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Roscovitine (CAS 186692-46-6)

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Alternate Names:
Seliciclib
Application:
Roscovitine is a potent and selective inhibitor of cyclin-dependent kinases. Selective for Cdk1, Cdk2, and Cdk5
CAS Number:
186692-46-6
Purity:
≥98%
Molecular Weight:
354.45
Molecular Formula:
C19H26N6O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Roscovitine is a potent and selective inhibitor of cyclin-dependent kinases which suppresses the proliferation of mammalian cell lines. Selective for Cdk1/cyclin B kinase (IC50=450nM), Cdk2 (IC50=700nM) and Cdk5/p35 (IC50=160nM). Roscovitine is more potent than olomoucine (sc-201526). It inhibits M phase promoting factor kinase activity and affects calcium channel gating. Roscovitine reversibly inhibits the transition from prophase to metaphase at micromolar concentrations in starfish oocytes and sea urchin embryos. It also inhibits in vitro M-phase-promoting factor activity and in vitro DNA synthesis in Xenopus egg extracts. A recent study shows that roscovitine inhibits Cdk5 kinase activity, cell proliferation, multicellular development, and Cdk5 nuclear translocation in Dictyostelium discoideum, without affecting the expression of Cdk5 protein during axenic growth. Roscovitine is an inhibitor of Cdk7, cyclin B, cyclin E, cyclin A, cyclin H, cdc2 and p53.


Roscovitine (CAS 186692-46-6) References

  1. The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis.  |  Whittaker, SR., et al. 2007. Cell Cycle. 6: 3114-31. PMID: 18075315
  2. Effect of seliciclib (CYC202, R-roscovitine) on lymphocyte alloreactivity and acute kidney allograft rejection in rat.  |  Pezzotta, A., et al. 2008. Transplantation. 85: 1476-82. PMID: 18497689
  3. R-roscovitine (Seliciclib) affects CLL cells more strongly than combinations of fludarabine or cladribine with cyclophosphamide: Inhibition of CDK7 sensitizes leukemic cells to caspase-dependent apoptosis.  |  Rogalińska, M., et al. 2010. J Cell Biochem. 109: 217-35. PMID: 19911397
  4. R-Roscovitine (Seliciclib) prevents DNA damage-induced cyclin A1 upregulation and hinders non-homologous end-joining (NHEJ) DNA repair.  |  Federico, M., et al. 2010. Mol Cancer. 9: 208. PMID: 20684776
  5. ATP-binding cassette B1 transports seliciclib (R-roscovitine), a cyclin-dependent kinase inhibitor.  |  Rajnai, Z., et al. 2010. Drug Metab Dispos. 38: 2000-6. PMID: 20699410
  6. The cyclin-dependent kinase inhibitor p57(Kip2) is epigenetically regulated in carboplatin resistance and results in collateral sensitivity to the CDK inhibitor seliciclib in ovarian cancer.  |  Coley, HM., et al. 2012. Br J Cancer. 106: 482-9. PMID: 22233925
  7. Characterization of cyclin E expression in multiple myeloma and its functional role in seliciclib-induced apoptotic cell death.  |  Josefsberg Ben-Yehoshua, L., et al. 2012. PLoS One. 7: e33856. PMID: 22558078
  8. Seliciclib, a cell-cycle modulator that acts through the inhibition of cyclin-dependent kinases.  |  Jackson, RC., et al. 2008. Expert Opin Drug Discov. 3: 131-43. PMID: 23480144
  9. Seliciclib inhibits renal hypertrophy but not fibrosis in the rat following subtotal nephrectomy.  |  Nutter, F., et al. 2012. Nephron Exp Nephrol. 122: 114-22. PMID: 23689642
  10. Modelling c-Abl Signalling in Activated Neutrophils: the Anti-inflammatory Effect of Seliciclib.  |  Jackson, RC. and Radivoyevitch, T. 2013. Biodiscovery. 7: 4. PMID: 24765523
  11. [Extrafocal osteosynthesis in treating infected defects of the tibia].  |  Buachidze, OSh., et al. 1977. Sov Med. 12-8. PMID: 867080
  12. Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine.  |  De Azevedo, WF., et al. 1997. Eur J Biochem. 243: 518-26. PMID: 9030780
  13. Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds.  |  Havlícek, L., et al. 1997. J Med Chem. 40: 408-12. PMID: 9046330

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Roscovitine, 1 mg

sc-24002
1 mg
$92.00

Roscovitine, 5 mg

sc-24002A
5 mg
$260.00

Hi, I would like to know whether Roscovitine you have with R-configuration (is it R-Roscovitine). Thanks

Asked by: Alhadidi
Thank you for your question. Yes, it's R-Roscovitine.
Answered by: Technical Support
Date published: 2019-04-13
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Rated 5 out of 5 by from Researchers report that by treating neuronsResearchers report that by treating neurons with roscovitine (CAS 186692-46-6) at increasing concentrations, a fourfold increase in Pak1 kinase activity was observed (PubMed ID # 9744280). -SCBT Publication Review
Date published: 2015-06-15
Rated 5 out of 5 by from BibbBibb, et. al. (PubMed ID # 10604473) reported that roscovitine (CAS 186692-46-6) reduced phospho-Thr75 DARPP-32 by 73% without affecting the total amount of DARPP-32. Simultaneously, roscovitine increased phospho-Thr34 DARPP-32 10 fold. -SCBT Publication Review
Date published: 2015-06-15
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Roscovitine is rated 5.0 out of 5 by 2.
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