Drug intelligence / Profile preview

Tyrphostin AG-17

Development stage
Discontinued
Lead developer
Molecule X
Modality
Small Molecules
Administration
Topical, Intravenous
01

Overview

Tyrphostin AG-17 (also known as RG-50872) is a synthetic small molecule belonging to the tyrphostin family of tyrosine kinase inhibitors. It was specifically developed to target the Platelet-Derived Growth Factor Receptor (PDGFR), inhibiting its autophosphorylation and downstream signaling pathways involved in cell proliferation and survival. In addition to its kinase inhibitory activity, AG-17 is recognized as a highly potent mitochondrial uncoupler (protonophore), which dissipates the mitochondrial membrane potential and disrupts oxidative phosphorylation. This dual functionality has led to its extensive use as a pharmacological tool in research concerning signal transduction, metabolic regulation, and hyperproliferative conditions. Although it was historically explored for therapeutic potential in treating psoriasis and preventing restenosis following angioplasty, development did not progress to clinical use, and it remains primarily a laboratory reagent.

Other names
3,5-Di-tert-butyl-4-hydroxybenzylidenemalononitrileTyrphostin 17Tyrphostin17Tyrphostin-17
02

Targets

PTK (Protein tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)

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