cenp-e

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。

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。

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.

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.

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