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HMN-176

Catalog No. T3643 CAS 173529-10-7

HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1).

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HMN-176, CAS 173529-10-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
500 mg	In stock	$ 1,190.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 98.99%

Purity: 97.95%

Biological Description

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Description	HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1).
In vitro	HMN-176 at a concentration of 2.5 μM significantly prolongs mitosis in hTERT-RPE1 and CFPAC-1 cell lines, independent of its impact on microtubule polymerization. Concentration-dependently, it inhibits aster formation at doses of 2.5, 0.25, and 0.025 μM. At varying concentrations (0.1, 1.0, or 10.0 µg/mL), HMN-176 exhibits inhibitory effects on breast, non-small-cell lung, and ovarian cancer specimens, with significant activity observed in 63% of breast, 67% of non-small cell lung, and 57% of ovarian tumor specimens treated at 10.0 µg/mL. It shows considerable cytotoxicity across different tumor types from various organs, with a mean IC50 value of 118 nM, indicating a broad cytotoxic effect. Furthermore, a 3 μM treatment of HMN-176 reduces MDR1 mRNA expression by 56%, although it does not significantly affect residual promoter activity.
In vivo	HMN-176 prevents spindle assembly and meiosis in Spisula oocytes by inhibiting centrosome-dependent MT nucleation, i.e., aster formation. Oocytes treated with 0.25 μM HMN-176 undergoes GVBD, but asters or spindles fails to form, even after prolonged periods[1]. After p.o. of HMN-214 to male rats, the prodrug is not detected in the plasma, while plasma levels of HMN-176 peaks at 2 h and gradually decreases thereafter[3].
Cell Research	Cells to be tested are seeded into a 96-well microplate at a density of 3 ×103-1×104 cells/well. Drugs are added the next day and the plate is incubated for 72 h at 37 °C in a humidified incubator (5% CO2, 95% air). The inhibition of growth is measuredby the MTT assay, and the concentration required to produce 50% inhibition of growth (IC50) calculated by the Scansoft 96 software program. The IC50 values for HMN-176 andreference agents are presented. Briefly, for each compound the mean IC50 value for all cell lines tested is calculated and the difference between the individual IC50 values and the mean IC50 value (log10) displayed by a bar projecting to the right or left of the mean. The resistance index is calculated as (IC50 value for drug-resistant cell line)/(IC50 for parent cell line).

Molecular Weight	382.43
Formula	C20H18N2O4S
CAS No.	173529-10-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (130.74 mM)

References and Literature

1. DiMaio MA, et al. The small organic compound HMN-176 delays satisfaction of the spindle assembly checkpoint by inhibiting centrosome-dependent microtubule nucleation. Mol Cancer Ther. 2009 Mar;8(3):592-601. 2. Medina-Gundrum L, et al. Investigation of HMN-176 anticancer activity in human tumor specimens in vitro and the effects of HMN-176 on differential gene expression. Invest New Drugs. 2005 Jan;23(1):3-9. 3. Takagi M, et al. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest New Drugs. 2003 Nov;21(4):387-99. 4. Tanaka H, et al. HMN-176, an active metabolite of the synthetic antitumor agent HMN-214, restores chemosensitivity to multidrug-resistant cells by targeting the transcription factor NF-Y. Cancer Res. 2003 Oct 15;63(20):6942-7.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Cell Cycle Compound Library Preclinical Compound Library Bioactive Compound Library NO PAINS Compound Library

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Keywords

HMN-176 173529-10-7 Cell Cycle/Checkpoint PLK HMN 176 Polo-like Kinase (PLK) HMN176 Inhibitor inhibit inhibitor

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