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Lucanthone

Cat. No. M20575
Lucanthone Structure
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Biological Activity

Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1.

Chemical Information
Molecular Weight 340.48
Formula C20H24N2OS
CAS Number 479-50-5
Solubility (25°C) DMSO 33 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Daniel P Radin, et al. Front Oncol. Lucanthone Targets Lysosomes to Perturb Glioma Proliferation, Chemoresistance and Stemness, and Slows Tumor Growth In Vivo

[2] Ji Yun Yoon, et al. Int J Mol Sci. Lucanthone, Autophagy Inhibitor, Enhances the Apoptotic Effects of TRAIL through miR-216a-5p-Mediated DR5 Upregulation and DUB3-Mediated Mcl-1 Downregulation

[3] Mei Wang, et al. Hum Reprod Update. Autophagy: a multifaceted player in the fate of sperm

[4] Mamta D Naidu, et al. PLoS One. Lucanthone and its derivative hycanthone inhibit apurinic endonuclease-1 (APE1) by direct protein binding

[5] Jennifer S Carew, et al. J Biol Chem. Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis

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Keywords: Lucanthone supplier, Autophagy, inhibitors, activators


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