Glycine, L-g-glutaMyl-S-(phenylMethyl)-L-cysteinyl-2-phenyl-,1,3-diethyl ester, (2R)-

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.

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.

Gutathione S-transferase