Description
Ezatiostat is an inhibitor of glutathione S-transferase pi 1-1 (GSTP1-1; K
i = 0.4 μM). It is selective for GSTP1-1 over GSTα and GSTμ family GSTs (K
is = 20-75 μM). Ezatiostat also inhibits the protein-protein interaction between GSTP1-1 and JNK1.
In vivo, ezatiostat (75 mg/kg) increases the number of circulating white blood cells in
Gstp1 wild-type, but not
Gstp1-/-, mice.
Uses
Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1, the most prevalent Glutathione S-transferases (GST) isozyme in nonhepatic tissues, catalytic activity with minimal effect on the related GSTα and -μ families.