Gutathione S-transferase

Gutathione S-transferase

Gutathione S-transferases (GSTs) are a diverse group of phase II drug metabolizing enzymes whose shared function is the conjugation of glutathione (GSH) to various electrophilic endo- and xenobiotics. A number of endogenously produced oxidized metabolites, such as propenal, 4-hydroxynonenals, organic hydroperoxides, phospholipids, and fatty acid peroxides, have been linked to GSTs.

The GST enzymes are divided into three distinct classes based on their subcellular localization, including membrane-bound microsomal, mitochondrial, and cytoplasmic. The cytosolic enzymes found in humans are the most prevalent and varied class of GSTs. These are referred to as phase II detoxification enzymes and include at least eight different isoenzymes, including alpha (A), kappa (K), mu (M), omega (O), pi (P), sigma (S), theta (T), and zeta (Z). In addition, bacteria, insects, and plants all contain members of the four distinct classes of this superfamily, known as beta, delta, phi, and tau.

Because certain isozymes are overexpressed in a variety of tumors and may contribute to the etiology of other illnesses like multiple sclerosis, asthma, and neurodegenerative diseases, GSTs have become a promising therapeutic target.

Gutathione S-transferase related products

Structure Cat No. Product Name CAS No. Product Description
V73166 7-Acetoxy-4-methylcoumarin (4-Methylumbelliferyl acetate) 2747-05-9 7-Acetoxy-4-methylcoumarin is a GST inhibitor.
V73167 BRD2889 1415153-39-7 BRD2889 is an analogue of the alkaloid piperamine.
V3435 Ezatiostat 168682-53-9 Ezatiostat (formerly known as TER199; TLK199; Brand name: Telentra) is a glutathione analog inhibitor ofglutathione S-transferase P1-1 (GSTP1-1).
V79667 GST-IN-1 GST-IN-1 (compound 16) is a glutathione S-transferase (GST) inhibitor (antagonist) with IC50s of 1.55 μM (sjGST) and 2.02 μM (hGSTM2).
V4571 GSTO1-IN-1 568544-03-6 GSTO1-IN-1, a chloroacetamide-containing compound, is a novel and potentglutathione S-transferase omega 1(GSTO1) inhibitor with anIC50of 31 nM.
V84246 GSTP1-1 inhibitor 1 3829-23-0
V73164 LAS17 2362527-67-9 LAS17 is a potent, irreversible, and selective inhibitor of glutathione S-transferase Pi (GSTP1).
V73165 TLK117 (TER117) 152684-53-2 TLK197 is the bioactive metabolite of TLK199, selectively inhibits glutathione S-transferase P1-1 (GSTP1-1), and binds GSTP with a Ki of 0.4 μM.
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