HMN-214

Alias: HMN214; HMN-214; HMN 214
Cat No.:V1577 Purity: ≥98%
HMN-214 (HMN 214; HMN214), stilbene derivative, is a potent and orally bioactive prodrug of HMN-176, which alters the cellular spatial orientation of Plk1 (polo-like kinase-1).
HMN-214 Chemical Structure CAS No.: 173529-46-9
Product category: PLK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

HMN-214 (HMN 214; HMN214), stilbene derivative, is a potent and orally bioactive prodrug of HMN-176, which alters the cellular spatial orientation of Plk1 (polo-like kinase-1). Poly-like kinase-1 (PLK1) is a serine/threonine kinase that controls important mitotic events. HMN-214 tampers with PLK1's subcellular geolocation. The mean IC50 of HMN-176 was 118 nM, indicating strong cytotoxicity. Furthermore, compared to other agents tested, HMN-176 was more cytotoxic toward drug-resistant phenotypes of tumor cells as indicated by its low resistance indices.

Biological Activity I Assay Protocols (From Reference)
Targets
PLK1
ln Vitro
HMN-214 is a prodrug of HMN-176. HMN-176 has a mean IC50 of 118 nM and exhibits strong activities against 22 human tumor cell lines[1]. In HeLa cells, HMN-176 (3-300 nM) dose-dependently suppresses luciferase expression regulated by the MDR1 promoter. Additionally, complex formation on the Y-box is dose-dependently suppressed by HMN-176 (30-3000 nM)[3]. In PC3-PSMA cells, HMN-214 (3.3 μM) increases luciferase expression 11-fold over vehicle control when using the 1,4C-1,4Bis polymer and 37-fold when using PEI. In MB49 cells, HMN-214 (≥ 3.3 μM) dramatically suppresses cell proliferation and causes notable morphological changes in the cells[4].
ln Vivo
HMN-214 (33 mg/kg, p.o.) converts to HMN-176 in rats. The aciatic and tibial nerves' action potential amplitude and conduction velocity are unaffected by HMN-214. In mice, HMN-214 (20 mg/kg, p.o.) shows antitumor activity[1]. HMN-214 (10, 20 mg/kg, p.o.) reduces the expression of MDR1 mRNA in tumor-derived KB and KB-A.1 in nude mice[3].
Enzyme Assay
HMN-214 is a potent and orally active prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
Cell Assay
The density of cells is seeded at 3 × 103–1 × 104 cells/well in a 96-well microplate. The plate is incubated for 72 hours after dilutions of HMN-214 or HMN-176 are added the following day. Following the MTT assay, IC50 values are obtained, which indicate the degree of growth inhibition.
Animal Protocol
Using an agate pestle, progressively add 0.5% methylcellulose 4000 solution to the ground HMN-214 to create a 3 mg/mL suspension. To get suspensions with the right concentration, this is further diluted with methylcellulose 4000 solution. By s.c. transplantation into naked mice, tumor tissue is grown beforehand. The resulting tumors are excised, cut into 8 mm3 cubic fragments, and then surgically transplanted subcutaneously using a trocar into the right axillary region of naked mice. On day 1, oral administration of HMN-214 is initiated once the tumor's theoretical volume has reached approximately 145 mm3.
References

[1]. 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.

[2]. A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors. Clin Cancer Res. 2006 Sep 1;12(17):5182-9.

[3]. 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.

[4]. Kinome-level screening identifies inhibition of polo-like kinase-1 (PLK1) as a target for enhancing non-viral transgene expression. J Control Release. 2015 Apr 28;204:20-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H20N2O5S
Molecular Weight
424.47
Exact Mass
424.11
Elemental Analysis
C, 62.25; H, 4.75; N, 6.60; O, 18.85; S, 7.55
CAS #
173529-46-9
Appearance
Solid powder
SMILES
CC(=O)N(C1=CC=CC=C1/C=C/C2=CC=[N+](C=C2)[O-])S(=O)(=O)C3=CC=C(C=C3)OC
InChi Key
OCKHRKSTDPOHEN-BQYQJAHWSA-N
InChi Code
InChI=1S/C22H20N2O5S/c1-17(25)24(30(27,28)21-11-9-20(29-2)10-12-21)22-6-4-3-5-19(22)8-7-18-13-15-23(26)16-14-18/h3-16H,1-2H3/b8-7+
Chemical Name
N-(4-methoxyphenyl)sulfonyl-N-[2-[(E)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide
Synonyms
HMN214; HMN-214; HMN 214
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: ~12 mg/mL (~28.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
0.5% methylcellulose: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3559 mL 11.7794 mL 23.5588 mL
5 mM 0.4712 mL 2.3559 mL 4.7118 mL
10 mM 0.2356 mL 1.1779 mL 2.3559 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.

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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.
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Biological Data
  • Dose-dependent enhancement of luciferase transgene expression by the PLK1 inhibitor HMN-214 in PC3-PSMA human prostate cancer and MB49 murine bladder cancer cells following delivery of pGL3.0 plasmid DNA using PEI and 1,4C-1,4Bis polymers. J Control Release . 2015 Apr 28:204:20-9.
  • Cell cycle analysis of PC3-PSMA cells treated with vehicle control (DMSO), 25 nM BI 2536, or 3.3 μM HMN-214 using flow cytometry and staining with propidium iodide (PI). J Control Release . 2015 Apr 28:204:20-9.
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