2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Glutathione S-transferase

Glutathione S-transferase

Glutathione transferases; GSTs

Glutathione S-transferase

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Glutathione 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. GSTs have been implicated in the conjugation of endogenously produced oxidized metabolites including propenal, 4-hydroxynonenals, organic hydroperoxides, phospholipids, and fatty acid peroxides.

On the basis of subcellular localization, the GST enzymes are grouped into three different classes namely, membrane-bound microsomal, mitochondrial and cytoplasmic. The leading and most diverse group of GSTs are the cytosolic enzyme spresent in humans. These are known as phase II detoxification enzymes that comprise of at least 8 classes of isoenzymes: alpha (A), kappa (K), mu (M), omega (O), pi (P), sigma (S), theta (T), and zeta (Z). In addition, four different classes of this superfamily, called beta (β), delta(δ), phi (Φ) and tau (τ) are also present in bacteria, insects and plants.

GSTs have emerged as a promising therapeutic target because specific isozymes are overexpressed in a wide variety of tumors and may play a role in the etiology of other diseases, including neurodegenerative diseases, multiple sclerosis, and asthma.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-A0122
    Plicamycin
    		Inhibitor 99.75%
    Plicamycin (Mithramycin A) is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein. Plicamycin inhibits GSTM2 promoter activity and protein expression.
    Plicamycin
  • HY-B1640
    Ethacrynic acid
    		Inhibitor 99.98%
    Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma.
    Ethacrynic acid
  • HY-13634A
    Ezatiostat
    		Inhibitor 99.19%
    Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.
    Ezatiostat
  • HY-111530
    GSTO1-IN-1
    		Inhibitor 99.47%
    GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.
    GSTO1-IN-1
  • HY-N1963
    Curzerene
    		Inhibitor 98.00%
    Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
    Curzerene
  • HY-160926
    16-Oxocafestol
    		Inducer ≥98.0%
    16-Oxocafestol enhances levels of glutathione S-transferase (GST) and tissue sulfhydryl in liver and in small bowel mucosa.
    16-Oxocafestol
  • HY-161876
    GSTO1-IN-2
    		Inhibitor
    GSTO1-IN-2 (Compound B-9) is a dual covalent inhibitor of GSTO1/BTK with IC50 values of 441 nM and 6.2 nM respectively.
    GSTO1-IN-2
  • HY-121624
    Anthglutin
    		Inhibitor
    Anthglutin is a gamma-glutamyltransferase inhibitor isolated from Penicillium oxalicum cultures. The Ki values ??of Anthglutin for different enzymes are: porcine kidney enzyme 5.7 μM, human kidney enzyme 18.3 μM, human liver soluble enzyme 13.6 μM, and conjugated enzyme 10.2 μM. Anthglutin had no significant effect on intestinal absorption of methionine in rats.
    Anthglutin
  • HY-B0766
    Bicyclol
    		99.91%
    Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.
    Bicyclol
  • HY-135318
    NBDHEX
    		Inhibitor 99.53%
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
    NBDHEX
  • HY-13634B
    TLK117
    		Inhibitor 99.89%
    TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
    TLK117
  • HY-115673
    LAS17
    		Inhibitor
    LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione?S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM. LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LAS17
  • HY-N1916
    Coniferyl ferulate
    		Inhibitor 98.56%
    Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST), reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 μM.
    Coniferyl ferulate
  • HY-112534
    GSTO-IN-2
    		Inhibitor ≥98.0%
    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.
    GSTO-IN-2
  • HY-126329
    AZD9898
    		Inhibitor 98.62%
    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.
    AZD9898
  • HY-N0548
    α-Angelica lactone
    		Activator 99.93%
    α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes.
    α-Angelica lactone
  • HY-117143
    TK05
    		Inhibitor 98.00%
    TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM.
    TK05
  • HY-B1640R
    Ethacrynic acid (Standard)
    		Inhibitor
    Ethacrynic acid (Standard) is the analytical standard of Ethacrynic acid. This product is intended for research and analytical applications. Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
    Ethacrynic acid (Standard)
  • HY-N7227
    Anonaine
    		Inhibitor
    Anonaine is an antiparasitic agent. Anonaine also is a glutathione S-transferase (GST) inhibitor.
    Anonaine
  • HY-N1282
    Seneciphylline
    		Activator 99.93%
    Seneciphylline is a toxic pyrrolizidine alkaloid in Gynura japonica. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities.
    Seneciphylline
Cat. No. Product Name / Synonyms Application Reactivity