Description | Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. | ||||||
---|---|---|---|---|---|---|---|
Targets |
| ||||||
In vitro | Treatment of HCT116 cells bohemine results in a 11% to 15% loss of cells from the S phase of the cell cycle with a 6% to 17% increase in the proportion of cells in the G2-M phase after 24 hours of treatment, as determined by propidium iodide staining and analysis by flow cytometry.Bohemine reduces RB phosphorylation at pharmacologically relevant concentrations that inhibit cell growth in cell culture[1]. | ||||||
In vivo | Given i.v., the single dose maximum tolerated dose for bohemine is 100 mg/kg. Following administration of 50 mg/kg i.v. bohemine to BALB/c− mice, Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h[1]. |