beta,beta-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 µM) and the main active component of Lithospermum erythrorhizon. beta,beta-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. beta,beta-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. beta,beta-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. beta,beta-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis[1][2][3][4].
Molekulargewicht:
370.40
Reinheit:
99.36
CAS Nummer:
[34539-65-6]
Formel:
C21H22O6
Target-Kategorie:
Apoptosis,CDK,FGFR,JNK,Necroptosis
Anwendungsbeschreibung:
MCE Product type: Natural Products
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