Gutathione S-transferase

Ezatiostat is a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity.

TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM.

AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma.

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.

GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.

TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1?C1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.