biological activity | NU6140 is a selective CDK2-cyclin A inhibitor (IC50,0.41 μM), and its selectivity is 10-36 times that of other CDK. NU6140 effectively inhibited the activity of Aurora A and Aurora B with IC50 values of 67 and 35 nM, respectively. Enhance the effect of inducing apoptosis and anti-tumor effect. |
target | cdk2-cyclin A 0.41 μ m (IC 50 ) CDK1-Cyclin B 6.6 μ m (IC 50 ) CDK4-Cyclin D 5.5 μ m (IC 50 ) cdk5-p25 15 μ m (IC 50 ) cdk7-cyclin H 3.9 μ m (IC 50 ) Aurora A 67 nm (IC 50 ) Aurora B 35 nm (IC 50 ) |
in vitro study | NU6140 is less active on CDK1-cyclin B, CDK4-cyclin d, CDK5-p25 and CDK7-cyclin h, with IC 50 s of 6.6, 5.5, 15 and 3.9 μ m, respectively. NU6140 increases catalytic activity of capase-9 and capase-3, uses increase in the sub-G1 apoptotic cell population. |