CENP-E-IN-1

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^[1]. In Vitro:CENP-E-IN-1 (Compound Cmpd-A) (200 nM; 3 h up to 12 h) induces pole-proximal chromosome misalignment, activates the SAC, and causes prolonged mitotic arrest in synchronized HeLa cells^[1].
CENP-E-IN-1 (0-1000 nM; 24-72 h) potently inhibits proliferation in asynchronous HeLa cells with a GI₅₀ of 80 nM, and its antiproliferative and pro-apoptotic effects are dependent on SAC activation via BubR1^[1].
CENP-E-IN-1 (3-3000 nM; 3 days) exhibits potent antiproliferative activity across a broad range of human cancer cell lines, though sensitivity is not correlated with CENP-E mRNA expression^[1]. In Vivo:CENP-E-IN-1 (100 mg/kg; i.p.; single dose) elevates tumor pHH3 levels, a marker of mitotic arrest in COLO205 xenograft nude mice^[1].
CENP-E-IN-1 (100 mg/kg; i.p.; three doses at 0, 8, and 24 hours on day 1) produces potent antitumor activity, with a T/C % of 11% on Day 8, in COLO205 xenograft nude mice without significant body weight loss^[1].