(R)-DRF053 dihydrochloride

Cat. No. 3610

(R)-DRF053 dihydrochloride C23H27N7O.2HCl [1241675-76-2]

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Chemical Name: 2-[[9-(1-Methylethyl)-6-[[3-(2-pyridinyl)phenyl]amino]-9H-purin-2-yl]amino]-1-butanol dihydrochloride

Biological Activity

Potent, ATP-competitive inhibitor of cyclin-dependent kinase (cdk) and casein kinase 1 (CK1) (IC50 values are 220, 80 and 14 nM for cdk1/cyclin B, cdk5/p25 and CK1 respectively). Selective over GSK-3 αβ (IC50= 4.1 μM). Also shown to inhibit amyloid-β production in N2A-APP695 cells.

Technical Data

M.Wt:
490.43
Formula:
C23H27N7O.2HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1241675-76-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 522.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for (R)-DRF053 dihydrochloride include:

Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046. PMID: 24740004.

Do you know of a great paper that uses (R)-DRF053 dihydrochloride from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: (R)-DRF053 dihydrochloride, supplier, casein, cyclin-dependent, kinases, cyclin, cdk5, cdk1, CK1, p25, dual, specificity, inhibits, inhibitors, Tocris Bioscience, Casein Kinase 1 Inhibitor products

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