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.
| 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. |
|
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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