1. Cell Cycle/DNA Damage
    Anti-infection
  2. DNA/RNA Synthesis
    Topoisomerase
    Parasite
  3. Hycanthone

Hycanthone 

Cat. No.: HY-B1099 Purity: 98.85%
Handling Instructions

Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.

For research use only. We do not sell to patients.

Hycanthone Chemical Structure

Hycanthone Chemical Structure

CAS No. : 3105-97-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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Description

Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent[1].

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

In Vitro

Hycanthone has an IC50 of 80 nM for inhibition of APE1 incision of depurinated plasmid DNA[1].
Hycanthone (0.05-100 µM; for 2 h) promotes APE1 cleavage in presence of Cycloheximide (CHX) and this cleavage is inhibited by 1% DMSO[1].
Hycanthone at 20 mg/mL or more is progressively more detrimental to cell viability. Results reveal that increased concentrations of Hycanthone, ranging from 0.1 to 10 μg/mL, progressively reduces viral interferon yields as much as 73% compare to that of controls[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Results show that the incorporation of tritiated thymidine into TCA-precipitable material of adult sensitive worms undergo a progressive decrease after treatment with Hycanthone. Immature worms are totally unaffected by Hycanthone at all times tested. Male worms treated with Hycanthone show signs of a possible partial recovery from the initial low levels of incorporation. The incorporation of tritiated leucine by drug-sensitive worms treated with Hycanthone is inhibited by 40 to 50% in the first four days after treatment. Results show that, 7 days after Hycanthone treatment, both ribosomal RNA species are reduced by at least 80% with respect to untreated worms, with some indication of a possible accumulation of heavier precursor molecules[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

356.48

Formula

C₂₀H₂₄N₂O₂S

CAS No.

3105-97-3

SMILES

O=C1C2=C(SC3=C1C=CC=C3)C(CO)=CC=C2NCCN(CC)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (35.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8052 mL 14.0260 mL 28.0521 mL
5 mM 0.5610 mL 2.8052 mL 5.6104 mL
10 mM 0.2805 mL 1.4026 mL 2.8052 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (3.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.25 mg/mL (3.51 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Appropriate quantities of Hycanthone (1 to 100 μg) in 10 mL maintenance medium are added to plastic flasks (75 cm2) containing approximately 3×107 LLC-MK2 cells in monolayer, which are then incubated at 35°C for 24 h. Maintenance medium is decanted, and 2 mL influenza virus is added onto cell monolayers and incubated at 35°C for 2 h. The multiplicity of infection is approximately 1.0. Inoculum is removed and 10 mL maintenance medium is added to each flask, which is then incubated at 35°C for 24 h. Supernatant fluid is decanted, centrifuged at 100,000 g for 1 h, dialyzed against HCI-KCI buffer (pH 2.0) at 4°C for 24 h, and then dialyzed against two changes of phosphate-buffered saline (pH 7.1) at 4°C for 24 h. Fluids are passed through filters to obtain sterile preparations. Samples are stored at -80°C until assayed for interferon activity[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female outbred Swiss albino mice used as definitive hosts weigh 18 to 20 g at the time of infection. Hycanthone is administered at 0.01 mL/g body weight intramuscularly by splitting the dose into the two hind legs, so that each mouse receives 80 mg/kg body weight of the free base. Treatments are usually performed during the 8th week after infection[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

HycanthoneDNA/RNA SynthesisTopoisomeraseParasitethioxanthenoneintercalatornucleicacidbiosynthesisapurinicendonuclease-1APE1Lucanthoneanti-schistosomalInhibitorinhibitorinhibit

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