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. |
|
V112320 | Bromodichloromethane | 75-27-4 | Bromodichloromethane is a common trihalomethane and a frequent byproduct of drinking water disinfection. |
|
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). |
|
V110278 | Glutathione-S-Transferase, Rat | Rat glutathione S-transferase (EC 2.5.1.18) is a phase II metabolic isoenzyme in eukaryotes and prokaryotes. Its most important function is to catalyze the binding of reduced glutathione (GSH) to exogenous substrates, thereby achieving detoxification. | |
|
V79667 | GST-IN-1 | 2987870-87-9 | 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). |
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V116032 | GSTA4-IN-1 | GSTA4-IN-1 (compound 3a) is a potent competitive inhibitor of glutathione S-transferase A4 (GSTA4) with an IC50 value of 3.12 μM and a Ki value of 2.38 μM. | |
|
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. |
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V117035 | GSTO1-IN-3 | 158890-32-5 | GSTO1-IN-3 is a potent GSTO1-1 inhibitor with an IC50 value of 0.11 μM and selectivity for GSTO2-2, GSTA1-1 and GSTP1-1 (IC50 > 100 μM). |
|
V117253 | GSTO1-IN-4 | 158890-33-6 | GSTO1-IN-4 is a selective and potent GSTO1-1 inhibitor (IC50 = 0.04 μM, KI = 0.16 μM). |
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V116761 | GSTO1-IN-5 | 2290641-22-2 | GSTO1-IN-5 is a potent and selective inhibitor of glutathione S-transferase ω1 (GSTO1) with an IC50 value of 0.22 nM. |
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V111084 | GSTO1-IN-6 | GSTO1-IN-6 is an allosterically covalently regulated GSTO1 inhibitor with an IC50 value of 457 nM. | |
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V84246 | GSTP1-1 inhibitor 1 | 3829-23-0 | |
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V116462 | KT53 | 1338494-49-7 | KT53 is a highly effective, selective, and cell-penetrating GSTO1 inhibitor. |
|
V73164 | LAS17 | 2362527-67-9 | LAS17 is a potent, irreversible, and selective inhibitor of glutathione S-transferase Pi (GSTP1). |
|
V119681 | ML175 | 610263-01-9 | ML175 is a specific inhibitor of glutathione transferase Omega 1-1 (GSTO1-1). |
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V112379 | Phorone | 504-20-1 | Phlorone (diisopropylideneacetone) is a glutathione (GSH) depleting agent. |
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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. |