β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor ( IC 50 =2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-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. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-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. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer , colistin-resistant bacterial infections, hepatitis and psoriasis.
Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > JNK | Products > Signaling Pathways > FGFR | Products > Signaling Pathways > Necroptosis | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > CDK
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