Kinesin-7/CENP-E Inhibitor

GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with K_i of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC₅₀ of 16.1 nM; PF-2771 is used as an anticancer agent.

Syntelin is a selective centromere protein E (CENP-E) inhibitor with IC₅₀ at 160 nM. Syntelin has antitumor activity.

CENP-E-IN-2 (compound 3) is a photoswitchable CENP-E inhibitor, with the pIC₅₀ of 6.82 without light illumination and 5.85 with 365 nm light illumination. CENP-E-IN-2 has antitumor activity.

CENP-E-IN-1 is a CENP-E inhibitor. CENP-E-IN-1 acts as a Mitotic arrest inducer and Apoptosis inducer, which causes abnormal alignment of chromosomes on the metaphase plate, activates the spindle assembly checkpoint and triggers apoptosis. CENP-E-IN-1 exhibits anti-tumor activity in colorectal adenocarcinoma xenograft models. CENP-E-IN-1 can be used in cancer-related research.

CENP-E-IN-3 (compound 4) is a potent CENP-E inhibitor. CENP-E-IN-3 has the potential for the research of cancer.