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.
Product information
CAS Number: 3105-97-3
Molecular Weight: 356.48
Formula: C20H24N2O2S
Chemical Name: 1-{[2-(diethylamino)ethyl]amino}-4-(hydroxymethyl)-9H-thioxanthen-9-one
Smiles: CCN(CCNC1=CC=C(CO)C2SC3C=CC=CC=3C(=O)C1=2)CC
InChiKey: MFZWMTSUNYWVBU-UHFFFAOYSA-N
InChi: InChI=1S/C20H24N2O2S/c1-3-22(4-2)12-11-21-16-10-9-14(13-23)20-18(16)19(24)15-7-5-6-8-17(15)25-20/h5-10,21,23H,3-4,11-13H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 12.5 mg/mL (35.07 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Hycanthone has an IC50 of 80 nM for inhibition of APE1 incision of depurinated plasmid DNA. Hycanthone (0.05-100 µM; for 2 h) promotes APE1 cleavage in presence of Cycloheximide (CHX) and this cleavage is inhibited by 1% DMSO. 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.
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.
Products are for research use only. Not for human use.
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