Daphnetin

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-1β, 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].

Product Specifications

CAS Number

[486-35-1]

Product Name Alternative

7,8-Dihydroxycoumarin

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Akt; AMPK; Apoptosis; Autophagy; Bcl-2 Family; Caspase; EGFR; mTOR; Parasite; PARP; PKA; PKC; Reactive Oxygen Species (ROS)

Type

Natural Products

Related Pathways

Anti-infection; Apoptosis; Autophagy; Cell Cycle/DNA Damage; Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Metabolic Enzyme/Protease; NF-κB; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Daphnetin.html

Purity

99.77

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic)

Smiles

O=C1C=CC2=CC=C(O)C(O)=C2O1

Molecular Formula

C9H6O4

Molecular Weight

178.14

Precautions

H302, H315, H319, H335

References & Citations

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