Tyrphostin A23 (CAS 118409-57-7)

Tyrphostin A23, also referred to as tyrphostin-23, is a member of a unique class of low molecular weight proteins known for their ability to inhibit protein tyrosine kinase and block the autophosphorylation of the EGF receptor. It can bind to the EGF receptor kinase domain with varying affinities and also inhibits PDGFR kinase. Tyrphostin A23 has been utilized in various scientific research applications to inhibit GP IIb-IIIa activation in permeabilized platelets, block calcium channel currents in vascular smooth muscle cells, enhance steroid-hormone secretion in human and rat adrenocortical cells, and inhibit the internalization of (125)I-transferrin in Heb7a cells. This compound, Tyrphostin A23, is a potent and reversible inhibitor of the epidermal growth factor receptor (EGFR) extensively utilized in both in vivo and in vitro scientific research applications. As a member of the tyrphostin family renowned for their ability to inhibit tyrosine kinase activity, Tyrphostin A23 specifically excels in suppressing EGFR activity, effectively modulating cellular signaling pathways and becoming useful in scientific investigations. Tyrphostin A23 exhibits a diverse range of biochemical and physiological effects. By inhibiting EGFR activity, it disrupts downstream signaling pathways, thereby impeding cell proliferation and differentiation. Moreover, Tyrphostin A23 demonstrates remarkable anti-inflammatory, anti-angiogenic, and anti-cancer properties. It effectively inhibits not only EGFR but also other tyrosine kinases such as the Src family of kinases. Additionally, it can hinder the activity of various proteins, including the transcription factor NF-κB and the protease caspase-3. The mechanism of action of Tyrphostin A23 involves binding to the ATP-binding pocket of EGFR, preventing the receptor from interacting with its ligands and consequently hindering its activity. This inhibition leads to the suppression of downstream signaling pathways, yielding diverse effects on cellular processes.