Date published: 2025-9-22

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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.

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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 CDK1/CDK5/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 References

  1. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases.  |  Bettayeb, K., et al. 2008. Oncogene. 27: 5797-807. PMID: 18574471
  2. Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1.  |  Oumata, N., et al. 2008. J Med Chem. 51: 5229-42. PMID: 18698753
  3. Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases.  |  Perez, DI., et al. 2011. Med Res Rev. 31: 924-54. PMID: 20577972
  4. Protein kinase CK1α regulates erythrocyte survival.  |  Zelenak, C., et al. 2012. Cell Physiol Biochem. 29: 171-80. PMID: 22415086
  5. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties.  |  Bibian, M., et al. 2013. Bioorg Med Chem Lett. 23: 4374-80. PMID: 23787102
  6. Physiology and pathophysiology of eryptosis.  |  Lang, F., et al. 2012. Transfus Med Hemother. 39: 308-14. PMID: 23801921
  7. Meta-Selective CAr-H Nitration of Arenes through a Ru3(CO)12-Catalyzed Ortho-Metalation Strategy.  |  Fan, Z., et al. 2016. J Am Chem Soc. 138: 8470-5. PMID: 27181121
  8. Inhibition of Cdk5 Promotes β-Cell Differentiation From Ductal Progenitors.  |  Liu, KC., et al. 2018. Diabetes. 67: 58-70. PMID: 28986398
  9. AGE-RAGE Axis Stimulates Oxidized LDL Uptake into Macrophages through Cyclin-Dependent Kinase 5-CD36 Pathway via Oxidative Stress Generation.  |  Yashima, H., et al. 2020. Int J Mol Sci. 21: PMID: 33291667
  10. Glucose-Dependent Insulinotropic Polypeptide Suppresses Foam Cell Formation of Macrophages through Inhibition of the Cyclin-Dependent Kinase 5-CD36 Pathway.  |  Terasaki, M., et al. 2021. Biomedicines. 9: PMID: 34356896

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Cdk/CKI Inhibitor, (R)-DRF053, 5 mg

sc-221408
5 mg
$209.00