Mitosis Activator

Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis.

P62-mediated mitophagy inducer (PMI) is a P62-mediated mitophagy activator. P62-mediated mitophagy inducer activates mitochondrial autophagy without recruitment of Parkin or collapse of the mitochondrial membrane potential and remains active in cells lacking a fully functional PINK1/Parkin pathway. P62-mediated mitophagy inducer serves as a pharmacological tool to study the molecular mechanisms of mitosis, avoiding toxicity and some of the non-specific effects associated with the sudden dissipation of mitochondria lacking membrane potential.

TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC₅₀s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.

(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth.

Head activator neuropeptide is a mitogen for mammalian cell lines of neuronal or neuroendocrine origin. Head activator neuropeptide signals by binding GPR37 and stimulates cells to enter mitosis.

Mps-BAY1 is an MPS1 inhibitor with anticancer activity. Mps-BAY1 inhibits cell proliferation and induces apoptosis by activating mitotic catastrophe in cancer cells, generating global aneuploidy and polyploidy. Mps-BAY1 can be used in the study of colorectal cancer and cervical cancer.

14,15-EET-SI is a sulfonimide (SI) analog metabolized from 14,15-EET, which is also an effective mitogen. 14,15-EET-SI can stimulate the incorporation of [3H] thymidine, activate pp60c-src and initiate the tyrosine kinase cascade, mediating their mitotic effects. Additionally, 14,15-EET-SI can increase cell proliferation as well as the expression of c-fos and egr-1 mRNA.

C-1311 shows to inhibit the catalytic activity of DNA topoisomerase II in vitro and in tumour cells. C-1311 prolongs G2 arrest followed by G2 to M transit and cell death during mitosis in the process of mitotic catastrophe.