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
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.)
Caractéristiques techniques
Marque
STEMCELL Technologies
Réf. B-LABO
BL-RE-151718
Réf. fabricant
17150272
CAS
212844-53-6
Synonyme
NG 60
Quantité
10 mg
Formule moléculaire
C<sub>19</sub>H<sub>25</sub>ClN<sub>6</sub>O
Pureté
≥98%
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