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CGP-74514A

Chemical Structure : CGP-74514A

CAS No.: 190653-73-7

CGP-74514A (CGP 74514A, CGP74514A)

Catalog No.: PC-61028Not For Human Use, Lab Use Only.

CGP-74514A is a cell permeable, potent, and selective inhibitor of CDK1/cyclin B with IC50 of 25 nM, and CLK1, CLK2, CLK4 inhibitor.

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    Biological Activity

    CGP-74514A is a cell permeable, potent, and selective inhibitor of CDK1/cyclin B with IC50 of 25 nM, and CLK1, CLK2, CLK4 inhibitor.
    CGP-74514A affects other kinases only at much higher concentrations (PKCα IC50=6.1 uM, PKA IC50=125 uM and EGFR IC50 >10 μM).
    CGP-74514A increases p21(CIP1) expression, p27(KIP1) degradation, diminishes E2F1 expression, and dephosphorylation of p34(CDC2) in U937 cells.
    CGP-74514A also is a potent CDC-like kinases inhibitor with IC50 of 148, 111 and 104 nM for CLK1, CLK2 and CLK4, respectively.

    Physicochemical Properties

    M.Wt 385.9
    Formula C19H24ClN7
    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

    N2-((1R,2S)-2-aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine

    References

    1. Shi Y, et al. Bioorg Med Chem Lett. 2017 Feb 1;27(3):406-412.

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