RoscovitineCAS: 186692-46-6
MF: C19H26N6O
MW: 354.45
A potent and selective inhibitor of cyclin-dependent kinases. Selective for Cdk1, Cdk2, and Cdk5.

Roscovitine (CAS 186692-46-6)

Roscovitine | CAS 186692-46-6 is rated 5.0 out of 5 by 2.
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Synonym: Seliciclib
Application: 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
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

1. Havlicek, L., et al. 1997. J. Med. Chem. 40: 408-412. PMID: 9046330
2. Rudolph, B., et al. 1996. EMBO J 15: 3065-3076. PMID: 867080
3. DeAzevado, W.F., et al. 1997. Eur. J. Biochem. 243: 518-526. PMID: 9030780
4. Buachidze, O.S.h., et al. 1977. Sov Med. : 12-18. PMID: 867080

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in chloroform (50 mg/ml), DMSO (5 mg/ml), water (0.3 mg/ml) at 25.0° C, ethanol (~10 mg/ml), DMF (~3 mg/ml), and 1:2 solution of ethanol:PBS (pH 7.2) (~0.3 mg/ml).
Storage :
Store at -20° C
Melting Point :
106-107° C
Boiling Point :
~577.5° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.64
IC50 :
CDK2/cyclin A : IC50 = 0.7 µM; CDK2/cyclin E: IC50 = 0.1 µM; CDK7/cyclin H: IC50 = 0.49 µM; CDK5/p35: IC50 = 0.16 µM; Cell division cycle (cdc)/cyclin B: IC50 = 0.65 µM; The growth of rapidly proliferating cells: IC50 = 15.2 µM; Reduced sensitivity towards ERK1: IC50 = 34 µM; Reduced sensitivity towards ERK2: IC50 = 14 µM; Proliferation of mammalian cell lines: IC50 = 16 µM
pK Values :
pKb: 4.77
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
160355
Merck Index :
14: 10240
MDL Number :
MFCD02266401
SMILES :
CC[[email protected]](CO)NC1=NC2=C(C(=N1)NCC3=CC=CC=C3)N=CN2C(C)C

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Roscovitine  Product Citations

See how others have used Roscovitine. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 25 total

PMID: # 30857869  Stretton, C.|Lipina, C.|Hyde, R.|Cwiklinski, E.|Hoffmann, TM.|Taylor, PM.|Hundal, HS.| et al. 2019. Biochim Biophys Acta Mol Cell Res.

PMID: # 30120810  Chen, XQ. et al. 2018. Traffic. 19: 840-853.

PMID: # 29606701  Pentimalli, F.|Forte, IM.|Esposito, L.|Indovina, P.|Iannuzzi, CA.|Alfano, L.|Costa, C.|Barone, D.|Rocco, G.|Giordano, A.| et al. 2018. Oncogene. 37: 3657-3671.

PMID: # 28450285  Li, FJ. et al. 2017. Am. J. Physiol. Lung Cell Mol. Physiol. 313: L80-L91.

PMID: # 28552936  Mohamed, NV. et al. 2017. PLoS ONE. 12: e0178288.

PMID: # 28904862  Momand, J.|Magdziarz, P.|Feng, Y.|Jiang, D.|Parga, E.|Celis, A.|Denny, E.|Wang, X.|Phillips, ML.|Monterroso, E.|Kane, SE.|Zhou, F.| et al. 2017. FEBS Open Bio. 7: 1328-1337.

PMID: # 26806339  Czapski, GA. et al. 2016. Neurochem. Int. 93: 103-12.

PMID: # 26788519  Draney, C. et al. 2016. J Diabetes Res. 2016: 6375804.

PMID: # 26188358  Zhou, W. et al. 2015. Oncotarget. 6: 21557-71.

PMID: # 25611431  Tian, XS. et al. 2015. CNS Neurosci Ther. 21: 398-409.

Citations 1 to 10 of 25 total

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 neurons Researchers 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 Bibb Bibb, 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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