| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| Targets |
PLK1
HMN-176 targets Polo-like kinase 1 (PLK1), a key regulator of mitosis. PLK1 is involved in various mitotic processes, including centrosome maturation, spindle assembly, and chromosome segregation. By inhibiting PLK1, HMN-176 disrupts these processes, leading to mitotic arrest and apoptosis in cancer cells. Its mechanism of action also involves interference with mitotic spindle formation. |
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| ln Vitro |
HMN-176 (2.5 μM) greatly increases the duration of mitosis in hTERT-RPE1 and CFPAC-1 Cell lines. Microtubule polymerization effects do not seem to be connected to spindle morphology effects of HMN-176. Aster formation is inhibited in a concentration-dependent manner by HMN-176 at 2.5, 0.25, and 0.025 μM[1]. Samples of ovarian, breast, and nonsmall-cell lung cancers show the greatest activity when exposed to HMN-176 (0.1, 1.0, or 10.0 µg/mL), which has inhibitory effects on a variety of tumors. 67% of non-small cell lung (4/6), 57% of breast (5/8), and 4/7 of ovarian tumor specimens treated with 10.0 µg/mL exhibit activity towards HMN-176[2]. The mean IC50 value of HMN-176 is 118 nM, indicating strong cytotoxicity. Regarding tumors with diverse features originating from different organs, HMN-176 exhibits comparable cytotoxicity[3]. Suppression of MDR1 mRNA expression by 56% occurs upon treatment with 3 μM HMN-176. On the residual promoter activity, HMN-176 has no discernible effect[4].
In vitro activity of HMN-176 is assessed in cell-based assays measuring mitotic arrest and apoptosis. Cancer cell lines are treated with the compound, and the accumulation of cells in mitosis is measured by flow cytometry using phospho-histone H3 staining. Apoptosis is measured by assessing caspase activation or Annexin V staining. |
| ln Vivo |
Plasma levels of HMN-176 peak at 2 hours and then progressively decline after p.o. of HMN-214 to male rats, but no prodrug is found in the plasma[3].
In vivo activity of HMN-176 has not been extensively reported. As a research compound, it may be evaluated in animal models of cancer to assess its antitumor efficacy. However, no specific in vivo data is available in the public domain. |
| Enzyme Assay |
The in vitro assay for HMN-176 typically involves cell-based assays measuring mitotic arrest. Cells are treated with varying concentrations of the compound, and the mitotic index is determined by flow cytometry using phospho-histone H3 (Ser10) staining or by microscopy. PLK1 activity can be assessed by measuring the phosphorylation of its substrates, such as Cdc25C, by Western blotting.
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| Cell Assay |
The test cells are seeded at a density of 3 ×103–1×104 cells/well into a 96-well microplate. The following day, medications are added, and the plate is kept in a humidified incubator with 5% CO2 and 95% air for 72 hours at 37 °C. The Scansoft 96 software calculates the concentration needed to produce 50% inhibition of growth (IC50), and the MTT assay is used to measure the amount of growth inhibition. The reference agents and HMN-176 IC50 values are shown. In summary, each compound's mean IC50 value across all tested cell lines is determined, and a bar projecting to the right or left of the mean indicates the difference between the IC50 values for each individual cell line and the mean IC50 value (log10). (IC50 value for drug-resistant cell line) / (IC50 for parent cell line) yields the resistance index.
Cellular assays for HMN-176 involve treating cancer cell lines with the compound and measuring its effects on the cell cycle and apoptosis. Cell cycle analysis is performed by flow cytometry using propidium iodide (PI) staining. Apoptosis is assessed by measuring caspase-3/7 activity, Annexin V staining, or by Western blotting for cleaved PARP. |
| Animal Protocol |
Male SD rats are given injections of 14C-HMN-214 and 14C-HMN-176 at doses of 33 (or 30 mg/kg of HMN-176) and 30 mg/kg, respectively. At predetermined times, blood samples are collected, and a liquid scintillation counter is used to measure the radioactivity levels in the plasma. Additionally, male rats are given unlabeled HMN-214 (33 mg/kg), and high performance liquid chromatography is used to measure the amounts of HMN-214 and HMN-176 in the plasma.
In vivo animal experiments for HMN-176 would typically involve administering the compound to mouse xenograft models of cancer. Tumor growth inhibition would be monitored, and pharmacodynamic markers, such as mitotic arrest and apoptosis induction in tumor tissue, would be assessed. However, no specific in vivo data is available. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for HMN-176 is not publicly available. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties would need to be characterized. Parameters such as oral bioavailability, half-life, and plasma protein binding would be determined.
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| Toxicity/Toxicokinetics |
HMN-176 is a research compound that is not intended for human use. Its toxicological profile has not been extensively characterized. Standard safety precautions should be followed when handling this compound in a laboratory setting.
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| References |
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| Additional Infomation |
HMN-176 is a research compound that inhibits mitosis and interferes with Polo-like kinase 1 (PLK1). It is used in studies of cancer and cell cycle regulation. The compound is available from various chemical suppliers for research purposes only.
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| Molecular Formula |
C20H18N2O4S
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| Molecular Weight |
382.432923793793
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| Exact Mass |
382.099
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| Elemental Analysis |
C, 62.81; H, 4.74; N, 7.33; O, 16.73; S, 8.38
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| CAS # |
173529-10-7
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| Related CAS # |
173529-10-7
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| PubChem CID |
12134997
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| Appearance |
White to off-white solid powder
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| LogP |
3.758
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
846
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC(=CC=1)OC)(N=C1C=CC=CC1=C/C=C1/C=CN(C=C/1)O)(=O)=O
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| InChi Key |
MYEJOKLXXLVMPR-STNHEDLKSA-N
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| InChi Code |
InChI=1S/C20H18N2O4S/c1-26-18-8-10-19(11-9-18)27(24,25)21-20-5-3-2-4-17(20)7-6-16-12-14-22(23)15-13-16/h2-15,23H,1H3/b17-7+,21-20+
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| Chemical Name |
(NE)-N-[(6E)-6-[2-(1-hydroxypyridin-4-ylidene)ethylidene]cyclohexa-2,4-dien-1-ylidene]-4-methoxybenzenesulfonamide
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| Synonyms |
HMN176; HMN-176; HMN 176
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 30 mg/mL (~78.5 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6149 mL | 13.0743 mL | 26.1486 mL | |
| 5 mM | 0.5230 mL | 2.6149 mL | 5.2297 mL | |
| 10 mM | 0.2615 mL | 1.3074 mL | 2.6149 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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