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MedChemExpress - Model Daphnetin -486-35-1

Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1?, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research[1][2][3][4].

Daphnetin

MCE China：Daphnetin

Brand：MedChemExpress (MCE)

Cat. No.HY-N0281

CAS：486-35-1

Synonyms：7,8-Dihydroxycoumarin

Purity：99.86%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1?, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.

In Vitro：Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells[1]. Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner[1]. Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway[1]. Daphnetin (7,8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner[3].

In Vivo：Daphnetin (7,8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft animal model[1]. Daphnetin (7,8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1[2]. Daphnetin (7,8-dihydroxycoumarin) (10-100 mg/kg; i.g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity in vivo[3].

IC50 & Target：EGFR 7.67 μM (IC50) Plasmodium PKA 9.33 μM (IC50) PKC 25.01 μM (IC50)

References：

[1]. Fan X, et, al. Daphnetin triggers ROS-induced cell death and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway in ovarian cancer. Phytomedicine. 2021 Feb;82:153465. [Content Brief]

[2]. Zhang L, et, al. Daphnetin protects against cisplatin-induced nephrotoxicity by inhibiting inflammatory and oxidative response. Int Immunopharmacol. 2018 Dec;65:402-407. [Content Brief]

[3]. Wang QM, et, al. The schizontocidal activity of daphnetin against malaria parasites in vitro and in vivo. Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 2000;18(4):204-6. [Content Brief]

[4]. Yang EB, Zhao YN, Zhang K, Mack P. Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor. Biochem Biophys Res Commun. 1999 Jul 14;260(3):682-5. [Content Brief]

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MedChemExpress - Model Daphnetin -486-35-1

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Daphnetin