cenp-e

PF-2771 是一种有效的，选择性的着丝粒蛋白 E (CENP-E) 抑制剂，IC50值为 16.1 nM。PF-2771具有抗肿瘤活性。

GSK923295 是一种特异性的变构着丝粒相关蛋白-E 驱动蛋白 ATPase 活性抑制剂，作用于人类和犬类此酶，Ki 分别为 3.2±0.2 nM 和 1.6±0.1 nM。

UMK57 是一种CENP-Ei、MCAK 增强剂，选择性促进 k-MT 附着错误纠正以抑制染色体错误分离的小分子化合物，可以通过破坏有丝分裂过程中动粒微管 (k-MT) 附着的稳定性来提高染色体分离保守性。

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

CENP-E-IN-3(compound 4)作为一种CENP-E抑制剂,展示出了显著的效果.该化合物在癌症研究领域显示出潜在的应用价值.

CENP-E-IN-2(compound 3)作为一种光控CENP-E抑制剂,其在无光照条件下的pIC50值为6.82,而在365 nm光照条件下的pIC50值达到5.85.此外,CENP-E-IN-2 还显示出抗肿瘤活性.

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.

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

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.