N-(cis-2-Aminocyclohexyl)-N-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine
CGP74514A Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable 2,6,9-substituted purine derivative that acts as a potent, selective inhibitor of Cdk1/cyclin B (IC50 = 25 nM). Reported to affect the activities of other kinases only at much higher concentrations (IC50 = 6.1 µM, 125 µM, and > 10 µM for PKCa, PKA, and EGFR, respectively). Shown to induce mitochondrial damage and apoptosis (≥ 3 µM) in several human leukemia cell lines. At lower concentrations (~1 µM), an initial G2M cell cycle arrest was observed in U937 cells, which eventually lead to apoptosis. Purity: ≥ 95% by HPLC. CAS 190654-01-4. Ref.: Yu. C., et al. 2003. Cancer Res. 63, 1822. Dai, Y., et al. 2002. Cell Cycle 1, 143. Imbach, P., et al. 1999. Bioorg. Med. Chem. Lett. 9, 91.
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