Hycanthone mesylate
Based on 2 publication(s) in Google Scholar
Hycanthone mesylate is an apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor, DNA intercalator and Antischistosomal agent, with an IC50 of 80 nM against APE1. Hycanthone mesylate irreversibly inhibits thymidine incorporation into DNA in adult sensitive *Schistosoma mansoni*, while exerts weak inhibitory effects on uridine and leucine incorporation. Hycanthone mesylate reduces influenza virus-induced interferon production. Hycanthone mesylate exhibits mutagenic effects in various organisms, shows teratogenicity in mice and rabbits, and induces neoplastic liver lesions in partially hepatectomized mice. Hycanthone mesylate can be used in research related to schistosomiasis and cancer.
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- CAS. Nr.: 23255-93-8
- Formel: C21H28N2O5S2
- Molecular Weight:452.58
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Publications Citing Use of MedChemExpress (MCE) Hycanthone mesylate
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Biologische Aktivität
Beschreibung
In Vitro
Hycanthone mesylate potently inhibits the endonuclease activity of APE1, with an IC50 of 80 nM[1].
Hycanthone (1.0-50.0 μg/mL; 24 h) mesylate reduces the viability of LLC-MK2 cells in a concentration-dependent manner, with a cell survival rate of 43.1% at 50.0 μg/mL, 78.8% at 20.0 μg/mL, and only extremely weak effects at concentrations ≤10.0 μg/mL[3].
Hycanthone (0.1-10.0 μg/mL; 24 h) mesylate potently inhibits influenza virus-induced interferon production in LLC-MK2 cells in vitro in a concentration-dependent manner, reducing interferon yield by 73.5% at a concentration of 10.0 μg/mL[3].
Hycanthone (24 h) mesylate does not alter interferon-mediated antiviral cellular resistance in clone 1-5c-4 cells[3].
Hycanthone (10.0 μg/mL) ethanesulfonate prevents IA-4 N-oxide from blocking its inhibitory effect on influenza virus-induced interferon production, reducing interferon yield by 78.0%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LLC-MK2
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Concentration:1.0 μg/mL; 5.0 μg/mL; 10.0 μg/mL; 20.0 μg/mL; 50.0 μg/mL
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Incubation Time:24 h
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Result:Maintains 100.7% surviving cells at 1.0 μg/mL relative to untreated controls.
Maintains 95.4% surviving cells at 5.0 μg/mL relative to untreated controls.
Maintains 91.7% surviving cells at 10.0 μg/mL relative to untreated controls.
Reduces surviving cells to 78.8% at 20.0 μg/mL relative to untreated controls.
Reduces surviving cells to 43.1% at 50.0 μg/mL relative to untreated controls.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:outbred Swiss albino mice (female, 18-20 g at infection, infected with Schistosoma mansoni hycanthone-resistant strain, treated at 8th week post-infection)[2]
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Dosage:80 mg/kg
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Administration:i.m.; single dose
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Result:Showed no inhibition of tritiated thymidine, tritiated/14C-labeled uridine, or tritiated leucine incorporation at any time tested.
Showed ribosomal RNA levels identical to those of untreated controls seven days after treatment.
Chemical Information
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CAS. Nr. 23255-93-8
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Molecular Weight 452.58
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Formel C21H28N2O5S2
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SMILES
O=C1C=2C=CC=CC2SC=3C(=CC=C(NCCN(CC)CC)C13)CO.O=S(=O)(O)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Anal Chem
Metal-Enhanced Aggregation-Induced Emission Strategy for the HIV-I RNA-Binding Ligand Assay. [Abstract]2022 Mar 22;94(11):4695-4702. PMID: 35258935 -
Biomol Ther (Seoul)
Hycanthone Inhibits Inflammasome Activation and Neuroinflammation-Induced Depression-Like Behaviors in Mice. [Abstract]2023 Mar 1;31(2):161-167. PMID: 36203404
Protokoll
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Reproductive and Developmental Toxicity Study
Reproductive and developmental toxicity studies detect adverse effects of prenatal or peri/postnatal exposure on maternal condition, pregnancy maintenance, embryo-fetal survival, fetal growth, structural development, and offspring reproductive or developmental endpoints; classic rat protocols generate readouts by comparing treated groups with vehicle, pair-fed, or untreated controls for implantation, resorption, fetal weight, crown-rump length, external morphology, visceral morphology, skeletal ossification, anogenital distance, nipple/areola retention, and postnatal cohort outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Reinheit & Dokumentation
Verweise
[1]. Naidu MD, et al. Lucanthone and its derivative hycanthone inhibit apurinic endonuclease-1 (APE1) by direct protein binding. PloS one. 2011;6(9):e23679. [Content Brief]
[2]. Pica Mattoccia L, et al. Effect of hycanthone administered in vivo upon the incorporation of radioactive precursors into macromolecules of Schistosoma mansoni. Molecular and biochemical parasitology. 1983 Jun;8(2):99-107. [Content Brief]
[3]. Hahon N, et al. Action of antischistosomal drugs, hycanthone and its analog 1A-4 N-oxide, on viral interferon induction. J Toxicol Environ Health. 1980 Jul;6(4):705-12. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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