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(R)-DRF053 dihydrochloride

Chemical Structure : (R)-DRF053 dihydrochloride

CAS No.: 1241675-76-2

(R)-DRF053 dihydrochloride (DRF 053;DRF053)

Catalog No.: PC-60582Not For Human Use, Lab Use Only.

(R)-DRF053 dihydrochloride (DRF053) is a potent, cell-permeable, dual CK1/CDK inhibitor with IC50 of 14 nM, 220 nM and 80 nM for CK1, CDK5/p25 and CDK1/cyclin B, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    (R)-DRF053 dihydrochloride (DRF053) is a potent, cell-permeable, dual CK1/CDK inhibitor with IC50 of 14 nM, 220 nM and 80 nM for CK1, CDK5/p25 and CDK1/cyclin B, respectively.
    (R)-DRF053 exhibits antiproliferative activity against human neuroblastoma SH-SY5Y cells with EC50 of 17.2 uM, prevents the CK1-dependent production of amyloid-beta in a cell model.
    (R)-DRF053 specifically increases the number of duct-derived β-cells without affecting their proliferation.

    Physicochemical Properties

    M.Wt 490.433
    Formula C23H29Cl2N7O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (R)-2-((9-isopropyl-6-((3-(pyridin-2-yl)phenyl)amino)-9H-purin-2-yl)amino)butan-1-ol dihydrochloride

    References

    1. Oumata N, et al. J Med Chem. 2008 Sep 11;51(17):5229-42.

    2. Zelenak C, et al. Cell Physiol Biochem. 2012;29(1-2):171-80.

    3. Liu KC, et al. Diabetes. 2018 Jan;67(1):58-70.

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