Mitosis Inhibitor

Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC₅₀=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (K_d= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.

Guanosine triphosphate-¹⁵N₅,d₁₄ dilithium (GTP-¹⁵N₅,d₁₄ dilithium) is the deuterated, ¹⁵N-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.

4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers.

Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC₅₀ of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells.

SSE15206 is a microtubule polymerization inhibitor (GI₅₀ = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.

Vincristine (sulfate) (Standard) is the analytical standard of Vincristine (sulfate). This product is intended for research and analytical applications. Vincristine sulfate (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a K_i of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine sulfate inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine sulfate upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine sulfate is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas.

(2S,3R)-Dap-NE hydrochloride is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity.

ELR510444 is an orally active tubulin inhibitor with an IC₅₀ of 10 μM. ELR510444 binds to the colchicine-binding site on β-tubulin, inhibits tubulin assembly, depolymerizes microtubules and blocks HIF activity. ELR510444 induces cellular microtubule loss, abnormal mitotic spindle, mitotic arrest, apoptosis, morphological changes in tumor endothelial cells, and inhibits cancer cell proliferation, angiogenesis and tumor growth. ELR510444 can be used in research related to various cancers such as renal cell carcinoma.

Guanosine triphosphate-d₁₄ dilithium (GTP-d₁₄ dilithium) is the deuterated-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.

(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles.

Estramustine phosphate, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer.

(E)-MS0019266 is a potent inhibitor of DNA damage repair. (E)-MS0019266 inhibits ribonucleotide reductase by generating reactive oxygen species. (E)-MS0019266 also reduces expression of genes related to cell cycle arrest and mitosis, including polo-like kinase 1, kinesin family member 20a, cyclin B1 and aurora kinase A. (E)-MS0019266 is promising for research of inhibitors of ribonucleotide reductase and polo-like kinase 1.

EAPB0503 is a quinoline compound with anti-tumor activity, showing strong cytotoxicity against melanoma cells in vitro (IC₅₀=200 nM). EAPB0503 can induce specific cell cycle arrest in mitosis of CML cells and directly activate apoptosis, leading to an increase in the G0 cell population, disruption of mitochondrial membrane potential, PARP cleavage, and DNA fragmentation. EAPB0503 also reduces the levels of BCR-ABL protein .

PDGFR Y1021 peptide (non-phosphorylation) is the non-phosphorylated fragment of platelet-derived growth factor receptor (PDGFR). PDGFR Y1021 peptide (non-phosphorylation) blocks the PLCγ association to PDGFR through PLCγSH2 domain, and thus inhibits mitogenic response.

ALB-109564 (12'-Methylthiovinblastine) hydrochloride, a tubulin inhibitor, is a cytotoxic agent designed to kill cancer cells by disrupting mitosis.

Cemadotin (LU103793) hydrochloride is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin hydrochloride blocks cells at mitosis, and exhibits K_i value of 1 μM for inhibiting tubulin. Cemadotin hydrochloride can be used to research anticancer.

GW837016X (NEU-391) is an orally active ErbB-2 kinase covalent inhibitor. GW837016X also is a potent antitrypanosome agent. GW837016X inhibits mitosis and cytokinesis.

S-72 inhibits tubulin polymerization and further triggers mitosis-phase cell cycle arrest and cell apoptosis, in addition to suppressing STAT3 signaling.

Vincristine-d₆ (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a K_i of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine sulfate inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine sulfate upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine sulfate is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas.

Tubulozole (R 46846) is an orally active inhibitor of tubulin polymerization with an ID₅₀ of 0.34 μM. Tubulozole induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole arrests Mitosis at the metaphase stage. Tubulozole causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole exerts anticancer activity against colon cancer. Tubulozole produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma.