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HMN-214 (IVX-214, HMN214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM. HMN-176 is an active metabolite of HMN-214 (IVX-214, HMN214). HMN-214 (IVX-214, HMN214) is an oral stilbene derivative. HMN-176 interferes with PLK1, but does not appear to directly inhibit PLK1. Instead, it alters its spatial distribution, resulting in cell cycle arrest at the G2–M phase, with destruction of the spindle polar bodies followed by DNA fragmentation. In human tumor xenografts, there was a broad spectrum of antitumor activity. The antitumor activity of HMN-214 (IVX-214, HMN214) was equal or superior to that of clinically available agents, including cisplatin, doxorubicin, vincristine, and tegafur-uracil.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr cells |
| Preparation method | Seeding cells into a 96-well microplate at a density of 3 × 103–1 × 104 cells/well. Adding dilutions of HMN-214 or HMN-176 the next day and incubating the plate for 72 hours. Using the MTT assay to measure cells and then obtaining IC50 values . |
| Concentrations | 0–10 μM, dissolved in DMSO |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Male BALB/c nude mice bearing xenografts of PC-3, A549, and WiDr cells |
| Formulation | Dissolved in 0.5% methylcellulose |
| Dosages | 10 mg/kg–20 mg/kg |
| Administration | Oral gavage on a QD ?28 schedule |
| Molecular Weight | 424.47 |
| Formula | C22H20N2O5S |
| CAS Number | 173529-46-9 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PLK Products |
|---|
| (1E)-CFI-400437 dihydrochloride
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). |
| 3MB-PP1
3MB-PP1 is a bulky purine analog and inhibitor of Polo-like kinase 1 (Plk1) that blocks mitotic progression and cytokinesis by targeting Plk1 in cells expressing the analog-sensitive Plk1 allele. 3MB-PP1 also specifically inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). 3MB-PP1 inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). In addition, 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits the Leu93 mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used in the mycelium of Candida albicans. 3MB-PP1 can be used in studies related to mycelium formation and cell division in Candida albicans. |
| CYC-800
CYC-800 is a PLK1 inhibitor that can be used in tumor-related studies. |
| SOL-686
SOL-686 is a PLK1 inhibitor that can be used in glioma-related studies. |
| BAL0891
BAL0891 is a potential first-in-class PLK1/TTK inhibitor with antiproliferative activity for studies related to solid tumors. |
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