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Potent casein kinase 1 (CK1) inhibitor (IC50 = 14 nM). Also an ATP-competitive cyclin-dependent kinase (cdk) inhibitor (IC50 values are 0.093 - 0.29, 0.21 and 0.82 μM for cdk2, cdk5 and cdk7, respectively). Shown to inhibit amyloid-β production in N2A-APP695 cells.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree 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|
References are publications that support the biological activity of the product.
Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 522
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
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Keywords: (R)-DRF053 dihydrochloride, (R)-DRF053 dihydrochloride supplier, casein, cyclin-dependent, kinases, cyclin, cdk5, cdk1, CK1, p25, dual, specificity, inhibits, inhibitors, Casein, Kinase, 1, Cyclin-dependent, 3610, Tocris Bioscience
1 Citation for (R)-DRF053 dihydrochloride
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
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