plk1 pbd

Plk1 PBD-IN-143 is a novel Inhibitor of the Polo-Box Domain of Polo-like Kinase 1 (Plk1 PBD).

Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.

T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

PLK1-IN-10 (Compound 4Bb), an orally active inhibitor of the PLK1 PBD (polo-box domain), inhibits the interaction between PLK1 and the cell division regulator protein 1 (PRC1) and reduces the protein expression of the CDK1-Cyclin B1 complex. Additionally, PLK1-IN-10 interacts with glutathione (GSH), enhancing cellular oxidative stress and promoting cell death [1].

Aristolactam AIIIa is a new type of Plk1 inhibitors, targeting the Polo Box domain (PBD), it has anti-tumor activity. Aristolactam IIIa shows inhibition of platelet aggregation induced by collagen or arachidonic acid.