A coumarin derivative with diverse biological activities; inhibits EGFR

Daphnetin – 50 mg

Brand:
Cayman
CAS:
486-35-1
Storage:
-20
UN-No:
Non-Hazardous - /

Daphnetin is a coumarin derivative that has been isolated from plants of the genus Daphne and has diverse biological activities, including kinase inhibitory, anti-proliferative, and antioxidative properties.{47032,47033,47034} It inhibits the EGF receptor (EGFR), PKA, and PKC (IC50s = 7.67, 9.33, and 25.01 µM, respectively, in kinase assays) and inhibits cell proliferation (IC50 = 73 µM) and reduces cyclin D1 levels in MCF-7 breast carcinoma cells.{47032,47033} Daphnetin (5 and 10 µg/ml) decreases the generation of reactive oxygen species (ROS) and production of malondialdehyde (MDA) and increases superoxide dismutase (SOD) activity and the glutathione (GSH) to oxidized GSH (GSSG) ratio in RAW 264.7 cells.{47034} It also prevents cytotoxicity and ROS overproduction induced by t-butyl hydroperoxide (t-BHP) in wild-type, but not Nrf2-/-, RAW 264.7 cells and increases the expression of proteins downstream of Nrf2, including HO-1, GCLM, GCLC, and NQO1.  

 

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Description

A coumarin derivative with diverse biological activities; inhibits EGFR, PKA, and PKC in vitro (IC50s = 7.67, 9.33, and 25.01 µM, respectively); inhibits cell proliferation (IC50 = 73 µM) in MCF-7 breast carcinoma cells; decreases the generation of ROS and production of MDA and increases SOD activity and the GSH:GSSG ratio in RAW 264.7 cells; prevents t-BHP-induced cytotoxicity and ROS overproduction in wild-type, but not Nrf2-/-, RAW 264.7 cells and increases the expression of proteins downstream of Nrf2

Formal name: 7,8-dihydroxy-2H-1-benzopyran-2-one

Synonyms:  7,8-Dihydroxycoumarin|NSC 633563

Molecular weight: 178.1

CAS: 486-35-1

Purity: ≥90%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Kinase Inhibitors|PKA||Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Natural Products|Coumarins||Product Type|Biochemicals|Ox Stress Reagents|Antioxidants||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|cAMP Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|Lipid Peroxidation||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen|Superoxide Dismutase||Research Area|Oxidative Stress & Reactive Species|Reactive Sulfur|Glutathione

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