1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Gutathione S-transferase

Gutathione S-transferase

Glutathione transferases; GSTs

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. 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.

Gutathione S-transferase Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-B1640
    Ethacrynic acid
    Inhibitor 99.98%
    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.
  • 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.
  • 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.
  • HY-N1963
    Curzerene
    Inhibitor
    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.
  • HY-13634B
    TLK117
    Inhibitor 98.18%
    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.
  • HY-149419
    GST-IN-1
    Inhibitor
    GST-IN-1 (compound 16) is a glutathione S-transferase (GST) inhibitor with IC50s of 1.55 μM (sjGST) and 2.02 μM (hGSTM2), respectively.
  • HY-N7227
    Anonaine
    Inhibitor
    Anonaine is an antiparasitic agent. Anonaine also is a glutathione S-transferase (GST) inhibitor.
  • HY-B1640A
    Ethacrynic acid sodium
    Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-N0548
    α-Angelica lactone
    Activator 98.08%
    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.
  • 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.
  • 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.
  • 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.
  • HY-N1282
    Seneciphylline
    Activator 99.88%
    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.
  • HY-117143
    TK05
    Inhibitor 98.00%
    TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM.
  • HY-145413
    BRD2889
    Inhibitor
    BRD2889 is an analog of the alkaloid piperlongumine. BRD2889 is a robust modulator of the GSTP1-ISCU axis in pulmonary hypertension (PH).
  • 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.
  • HY-108538
    Ethacrynic acid D5
    Inhibitor
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic 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.
  • HY-13634
    Ezatiostat hydrochloride
    Inhibitor
    Ezatiostat hydrochloride (TER199; TLK199 hydrochloride) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat hydrochloride leads to JNK activation by inhibiting GSTP1. Ezatiostat hydrochloride stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat hydrochloride has the potential for myelodysplastic syndrome (MDS) treatment.