(R)-DRF053 dihydrochloride

Catalog # Availability Size / Price Qty
(R)-DRF053 dihydrochloride | CAS No. 1241675-76-2 | Casein Kinase 1 Inhibitors
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Description: Potent CK1 inhibitor; also inhibits cyclin-dependent kinases

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

Purity: ≥98%

Product Details
Citations (1)

Biological Activity

(R)-DRF053 dihydrochloride is a 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.

Technical Data

Soluble to 100 mM in water and to 100 mM in DMSO
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.

Background References

  1. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
    Jorda et al.
    J.Med.Chem., 2018;61:9105
  2. Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1.
    Oumata et al.
    J.Med.Chem., 2008;51:522

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Citation for (R)-DRF053 dihydrochloride

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

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