PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor. PF-2771 inhibits CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 is used as an anticancer agent.

CENP-E:16.1 nM

PF-2771 is a potent and selective CENP-E inhibitor, inhibiting CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 shows no inhibitory effect on the ATPase activities of highly related kinesins (0% inhibition of Eg5/KSP, chromokinesin, and MCAK at both 1 or 10 μM PF-2771). PF-2771 exhibits inactive activity against 74 protein kinases (all < 23% inhibition with 1 μM PF-2771, < 40% with 10 μM PF-2771). PF-2771 is cytotoxic to the basal-like breast cancer tumor cell survival, with EC 50 s of < 0.1 μM, and with no cytotoxicity on the normal and premalignant cell lines (EC 50 > 5 μM). PF-2771 (100 nM) causes a chromosomal congression defect in MDA-MB-468 cells [1].

PF-2771 (100 mg/kg, every day i.p.) potently inhibits CENP-E motor function, and leads to tumor regression in SCID mice bearing AA1077 mammary tumors [1].