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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
7-Acetoxy-4-methylcoumarin (4-Methylumbelliferyl acetate) V73166 7-Acetoxy-4-methylcoumarin (4-Methylumbelliferyl acetate) 2747-05-9 7-Acetoxy-4-methylcoumarin is a GST inhibitor.
BRD2889 V73167 BRD2889 1415153-39-7 BRD2889 is an analogue of the alkaloid piperamine.
Bromodichloromethane V112320 Bromodichloromethane 75-27-4 Bromodichloromethane is a common trihalomethane and a frequent byproduct of drinking water disinfection.
Ezatiostat 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).
Glutathione-S-Transferase, Rat 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.
GST-IN-1 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).
GSTA4-IN-1 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.
GSTO1-IN-1 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.
GSTO1-IN-3 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).
GSTO1-IN-4 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).
GSTO1-IN-5 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.
GSTO1-IN-6 V111084 GSTO1-IN-6 GSTO1-IN-6 is an allosterically covalently regulated GSTO1 inhibitor with an IC50 value of 457 nM.
GSTP1-1 inhibitor 1 V84246 GSTP1-1 inhibitor 1 3829-23-0
KT53 V116462 KT53 1338494-49-7 KT53 is a highly effective, selective, and cell-penetrating GSTO1 inhibitor.
LAS17 V73164 LAS17 2362527-67-9 LAS17 is a potent, irreversible, and selective inhibitor of glutathione S-transferase Pi (GSTP1).
ML175 V119681 ML175 610263-01-9 ML175 is a specific inhibitor of glutathione transferase Omega 1-1 (GSTO1-1).
Phorone V112379 Phorone 504-20-1 Phlorone (diisopropylideneacetone) is a glutathione (GSH) depleting agent.
TLK117 (TER117) 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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