Cdk/CKI Inhibitor, (R)-DRF053 MF: C23H27N7O H2O
MW: 435.5
An inhibitor of CDK1/CDK5/CK1 activity while maintaining selectivity against GSK-3α/β.

Cdk/CKI Inhibitor, (R)-DRF053

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Application: Cdk/CKI Inhibitor, (R)-DRF053 is an inhibitor of CDK1/CDK5/CK1 activity while maintaining selectivity against GSK-3α/β
Molecular Weight: 435.5
Molecular Formula: C23H27N7O H2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cdk/CKI Inhibitor, (R)-DRF053 is a cell-permeable ATP-binding pocket-targeting (R)-Roscovitine derivative that is more potent than Roscovitine in inhibiting Cdc2 (CDK1)/CDK5/Casein Kinase (CK1) activity while maintaining selectivity against GSK-3α/β. The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells. Cdk/CKI Inhibitor, (R)-DRF053 is an inhibitor of cyclin B and p35.


References

1. Oumata, N., et al. 2008. J. Med. Chem. 51: 5229-5242. PMID: 18698753
2. Bettayeb, K., et al. 2008. Oncogene. 27: 5797-5807. PMID: 18574471

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mg/ml), and ethanol (30 mg/ml).
Storage :
Store at 4° C
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
CK1 activity: IC50 = 14 nM; CDK5 activity: IC50 = 80 nM; CDK1 activity: IC50 = 220 nM; GSK-3α/β: IC50 = 4.1 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
MDL Number :
MFCD14585501
SMILES :
CC[[email protected]](CO)NC1=NC2=C(C(=N1)NC3=CC=CC(=C3)C4=CC=CC=N4)N=CN2C(C)C.O

Download SDS (MSDS)

Certificate of Analysis

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Cdk/CKI Inhibitor, (R)-DRF053  Product Citations

See how others have used Cdk/CKI Inhibitor, (R)-DRF053. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 18574471  Bettayeb, K. et al. 2008. Oncogene. 27: 5797-5807.

PMID: # 18698753  Oumata, N. et al. 2008. J. Med. Chem. 51: 5229-5242.

Citations 1 to 2 of 2 total
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