cenp-e

GSK923295 is a selective allosteric inhibitor of CENP-E kinesin motor ATPase(Ki=3.2 nM).

CENP-E-IN-3 (compound 4) is an effective inhibitor of CENP-E with potential applications in cancer research.

CENP-E-IN-2 (compound 3) is a photocontrollable CENP-E inhibitor exhibiting a pIC50 of 6.82 in the absence of light and a pIC50 of 5.85 under 365 nm light exposure. This compound also demonstrates antitumor activity.

UMK57 is a CENP-Ei and MCAK enhancer, selectively promoting k-MT attachment error correction to inhibit chromosome missegregation of small molecule compounds, and can improve chromosome separation conservation by disrupting the stability of kinetosomal microtubule (k-MT) attachment during mitosis.

Cmpd-A is a time-dependent CENP-E inhibitor with potent antitumor activity. Cmpd-A inhibits the ATPase activity of the CENP-E motor domain, acting as a time-dependent inhibitor with an ATP-competitive-like behavior. Cmpd-A causes chromosome misalignment on the metaphase plate, leading to prolonged mitotic arrest. Treatment with Cmpd-A induces antiproliferation in multiple cancer cell lines.

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

Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. Tcherniuk et al (2011) UA62784 is a cytotoxic inhibitor of microtubules, not CENP-E. Chem.Biol. 18 631 PMID:21609844 |Maiato and Logarinho et al (2011) Motor-dependent and -independent roles of CENP-E at kinetochores: the cautionary tale of UA62784. Chem.Biol. 18 679 PMID:21700202

MS 347a is a myosin light chain kinase (MLCK) inhibitor; an epoxide analog of sydowinin B (MS-347b).

Syntelin is a selectively CENP-E inhibitor. Syntelin inhibited CENP-E motility in a dose-dependent manner with an IC50 value of 160 nM. Among an extensive list of mitotic kinesins examined, syntelin was found to be highly selective for CENP-E. Syntelin binds to different sites from those of GSK923295, a recently identified CENP-E ATPase inhibitor, as syntelin inhibits CENP-E mutants resistant to GSK923295 in a manner indistinguishable from that of wild type motor. Syntelin represents a novel class of CENP-E motor inhibitor.