mitotic

BRD9876 is a selective inhibitor of MM1S growth.

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

Colcemid (NSC-3096) is a microtubule polymerization inhibitor, with the main target being Tubulin and an IC50 of 2.4 μM. Colcemid can induce apoptosis and can be used in the research of tumors and embryo cloning.

Maytansine (NSC-153858), an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata, inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

TC11 (1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11) is a potent inhibitor of tumor cell proliferation and an inducer of apoptosis via activation of caspase-3, 8 and 9.

Scoulerine is an inhibitor of ß-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

cis-trismethoxy Resveratrol ((Z)-3,5,4'-Trimethoxystilbene) inhibits tubulin polymerization (IC50 = 4 μM) and has anti-mitotic effects.

FiVe1 is a vimentin binding small molecule that promotes the disintegration and phosphorylation of vimentin in the metaphase, leading to mitotic disasters, polynuclearization, and loss of cancer cell dryness. FiVe1 selectively and irreversibly inhibit the growth of mesenchymal transformed breast cancer cells (FOXC2-HMLER cell, IC50=234nM) and soft tissue sarcomas of different histological subtypes.

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

Chloroxine (Capitrol) is a synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.

Maleuric acid (N-Carbamoylmaleamic acid) is anti-mitotic and can be used in biological research in conjunction with radioautography.Maleuric acid is used to improve the growth and fertility of plants and animals as well as to treat whey acid deficiency.

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

4-tert-Octylphenol, an endocrine-disrupting chemical with estrogenic properties, notably induces apoptosis in offspring mouse brain neuronal progenitor cells. This compound decreases levels of bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), thereby diminishing the proliferation of neuronal progenitors. Consequently, 4-tert-Octylphenol adversely affects brain development and behavior in mice.

Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antidiarrhoeic, antilipolytic, antispasmodic, and anti-tumor properties. Zingerone (Gingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways, acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.

PAIB-SOs-12 is an anti-mitotic compound that shows anti-proliferative activity at low concentrations and induces cytoskeletal damage in MCF7 cells.

LQZ-7F is a small molecule survivin dimerisation inhibitor with anticancer activity.LQZ-7F induces proteasome-dependent survivin degradation, mitotic arrest, and apoptosis, and blocks human tumour growth in mouse xenograft assays.

Tubulin polymerization-IN-47 is a tubulin polymerization inhibitor and mitotic inhibitor with antitumor activity and inhibitory effects on neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell lines, respectively. Tubulin polymerization-IN-47 is a candidate compound for the treatment of hepatocellular carcinoma, colon cancer, lung cancer and breast cancer.

Vinorelbine (KW-2307 base) is a semisynthetic vinca alkaloid. Vinorelbine binds to tubulin and prevents the formation of the mitotic spindle, resulting in the arrest of tumor cell growth in metaphase.

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A/-B/-C with Kd values ranging from 23-289 nM.

CP5V, a PROTAC, induces mitotic inhibition, and suppresses cancer cell proliferation. It specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation.