CDK1/2InhibitorIII

Uses

Cyclin-dependent kinases (CDKs) are protein kinases and involved with the regulation of the cell cycle. CDK 1/2 inhibitor III selectively inhibits CDK1 and CDK2. Studies have shown that CDK 1/2 Inhibitor III can also inhibit in vitro cellular proliferation in various human tumor cells.

Uses

Cyclin-dependent kinases (Cdks) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Cdk1/2 Inhibitor III is a cell-permeable inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50s = 0.6 and 0.5 nM, respectively). It less potently inhibits CDC2-like kinases 1 and 3, VEGFR2, and GSK-3β (IC50s = 8.9, 29, 32, and 140 nM, respectively) and is without effect against a panel of other kinases. Cdk1/2 Inhibitor III blocks the growth of several cancer cell lines (IC50 values range from 20 to 92 nM).

General Description

A cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC₅₀ = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Acts as a highly potent, reversible, ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC₅₀ = 600 pM and 500 pM, respectively) with selectivity over VEGF-R2 (IC₅₀ = 32 nM), GSK-3β (IC₅₀ = 140 nM), and a panel of eight other kinases (IC₅₀ ≥ 1 μM).

Biochem/physiol Actions

Cell permeable: yes