Purvalanol A
Cyclin/CDK pathway inhibitor; Inhibits CDKs
Purvalanol A
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Purvalanol A is a cell-permeable, potent, and selective inhibitor of cyclin-dependent kinases (CDKs). CDKs and cyclins form a stoichiometric complex which is necessary for the CDK subunit to gain its protein kinase activity. It has been shown that these CDK/cyclin complexes play a key role in initiating G2/M transitions of the cell cycle (Jackman & Pines). Purvalanol A acts through competitive inhibition of ATP binding, to inhibit CDK1/cyclin B (IC₅₀ = 4 nM), CDK2/cyclin A (IC₅₀ = 70 nM), CDK2/cyclin E (IC₅₀ = 35 nM), CDK4/cyclin D1 (IC₅₀ = 850 nM) and CDK5-p35 (IC₅₀ = 75 nM; Bain et al.; Gray et al.), thereby arresting cells in G1 and G2.
CANCER RESEARCH
- Inhibits proliferation in exponentially growing cancer cell lines and reversibly arrests synchronised cells in G1 and G2 phase of cell cycle (Villerbu et al.).
- Induces apoptosis in MCF-7 estrogen receptor positive breast cancer cells (Obakan et al.).
- Suppresses cancer progression associated with Src up-regulation by the coordinated inhibition of cell cycle progression and tyrosine kinase signaling (Hikita et al.).
