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.
Compound Libraries
(R)-DRF053 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 490.43 |
| Formula | C23H27N7O.2HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1241675-76-2 |
| PubChem ID | 71433624 |
| InChI Key | BQPRBNGSDBTKAK-ZEECNFPPSA-N |
| Smiles | CC(C)N2C1=NC(N[C@H](CC)CO)=NC(NC3=CC(C4=NC=CC=C4)=CC=C3)=C1N=C2.Cl.Cl |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.04 | 100 | |
| water | 49.04 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 490.43. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.04 mL | 10.2 mL | 20.39 mL |
| 5 mM | 0.41 mL | 2.04 mL | 4.08 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 522 PMID:
Keywords: (R)-DRF053 dihydrochloride, supplier, casein, cyclin-dependent, kinases, cyclin, cdk5, cdk1, CK1, p25, dual, specificity, inhibits, inhibitors, Casein, Kinase, 1, Cyclin-dependent, Kinase, Casein, Kinase, 1, Tocris Bioscience
