metaphase

Colcemid (NSC-3096) is a microtubule polymerization inhibitor that primarily targets tubulin, with an IC₅₀ of 2.4 μM. Demecolcine interacts with tubulin dimers, induces antimitotic effects, and inhibits microtubule growth. Colcemid is a classic reagent used in karyotyping, banding techniques, and cell cycle synchronization. Colcemid can induce apoptosis and is used in studies of tumor and embryonic cloning.

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.

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.

A-259745 is an orally active antimitotic agent that binds to the colchicine site on tubulin. It exhibits potent in vitro cytotoxic activity against both multidrug-resistant and non-multidrug-resistant cancer cell lines, with ED50 values of 0.018 μM for HCT-15 and 0.028 μM for NCI-H460 cells. A-259745 inhibits tubulin polymerization, disrupting the dynamic equilibrium of the mitotic spindle, causing dividing cells to arrest in the metaphase-anaphase transition, which subsequently induces apoptosis (apoptosis). In mouse tumor models, A-259745 demonstrates dose-dependent antitumor efficacy and is useful for cancer research.

LY195448 HCl is a phenethanolamine shown anti-tumour activity. It blocks cells at metaphase.

Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.3 sequence and is biotinylated via a C-terminal GK linker. Unlike histone H3.1 and H3.2, the histone H3.3 variant contains a serine residue at position 31 that is phosphorylated during late prometaphase and metaphase of mitosis. Histone H3 (21-44) also contains lysine residues at positions 23, 27, and 36 that are subject to methylation and acetylation, all of which have a role in the regulation of gene expression, and a serine residue at position 28 that is subject to phosphorylation during mitosis.

Myrmicacin is an inhibitor of mitotic progression after metaphase.

Cmpd-A is a time-dependent inhibitor of Centromere-associated protein E (CENP-E). It inhibits ATPase activity and exhibits an ATP-competitive-like behavior. In cellular models, Cmpd-A causes chromosome misalignment and leads to mitotic arrest, thereby inhibiting tumor cell proliferation.

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

FF-MAS is a potent agonist that enhances the meiotic maturation and preimplantation development of mouse oocytes cultured in vitro. It facilitates progression to metaphase II (MII) and augments the oocytes' ability to advance from the 2-cell stage to the blastocyst transition [1] [2].

Vincristine-D3-ester sulfate istine-D3-ester (sulfate) is the deuterated form of Vincristine sulfate. Vincristine sulfate, an antineoplastic vinca alkaloid, inhibits the formation of microtubules in mitotic spindles, leading to cell cycle arrest at metaphase. It binds to microtubules with a Ki of 85 nM.

Vincristine-D3 sulfate is the deuterated form of Vincristine sulfate. Vincristine sulfate (T1270) is an antitumor vinca alkaloid that inhibits the formation of microtubules in the mitotic spindle, resulting in the arrest of dividing cells at metaphase. It binds to microtubules with a Ki of 85 nM.