PLK

BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.

BI6727 is a highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines).

GSK461364 is an ATP-competitive inhibitor of polo-like kinase 1 (Plk1).

HMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts.

ON-01910 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress.

GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively).

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.

Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.

NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity.

SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively).

LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 uM; also inhibits PLK3 with IC50 of 7.2 uM.

Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle.

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.