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Erbstatin

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101006

    EGFR Cancer
    Methyl 2,5-dihydroxycinnamate is an erbstatin analog and a stable, potent inhibitor of EGFR kinase activity .
    Methyl 2,5-dihydroxycinnamate
  • HY-113549

    EGFR Apoptosis Cancer
    Erbstatin, a EGFR kinase inhibitor, possesses antineoplastic effect .
    Erbstatin
  • HY-118175

    Others Others
    RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
    RG 14921

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