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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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Purity & Documentation Purity: >98% (HPLC)

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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