Glutathione S-transferase Inhibitor

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.

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.

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.

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.

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.

Piriprost potassium (U 60257B) is an inhibitor of Glutathione-S-transferase and leukotriene biosynthesis inhibitor. Piriprost potassium inhibits the biosynthesis of leukotriene C/D without affecting cyclooxygenase-mediated arachidonic acid metabolites. Piriprost potassium increases the activity of alkaline phosphatase (ALP). Piriprost potassium antagonizes contractions induced by leukotriene C/D in vitro. Piriprost potassium is used in asthma research.

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC₅₀ of 31 nM.

Aviglycine hydrochloride (ABG-3168) is an inhibitor of ethylene biosynthesis. The use of Aviglycine hydrochloride (ABG-3168) delays the natural flowering of pineapples, reduces fruit drop, and maintains fruit firmness.

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.

Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC₅₀ = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.

TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a K_i of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a K_i of 0.56 μM.

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.

TK05 is a potent and selective inhibitor of leukotriene C₄ synthase (LTC4S) with an IC₅₀ of 95 nM.

Noreugenin is a phenolic compound found in Calea uniflora Less. Noreugenin inhibits myeloperoxidase activity and reduces levels of proinflammatory cytokines IL-1β and IL-17A levels in LPS (HY-D1056)-induced murine pleurisy model. Noreugenin reduces apoptosis and necrosis. Noreugenin reduces lipid peroxidation, and antioxidant enzyme (CAT, SOD, GST) activity. Noreugenin exhibits anti-inflammatory and antioxidant effects. Noreugenin can be used for the research of inflammatory conditions, such as pleurisy.

Methyl orsellinate acts as an antiviral agent and insecticide. Methyl orsellinate exhibits enzyme inhibitory activity, with an IC₅₀ of 59.6 µM against porcine leukocyte 5-lipoxygenase (5-LOX); it inhibits soybean 15-lipoxygenase (15-LOX), and shows weak inhibitory activity against acetylcholinesterase (AChE) and glutathione S-transferase (GST). Methyl orsellinate displays contact toxicity against adult Drosophila suzukii. Methyl orsellinate shows anti-HSV-1 activity. Methyl orsellinate can be used in studies related to *Drosophila suzukii* infestation and HSV-1 infection.

Anonaine is an antiparasitic agent. Anonaine also is a glutathione S-transferase (GST) inhibitor.

ML175 is a specific glutathione transferase Omega 1-1 (GSTO1-1) inhibitor. ML175 can significantly activate Akt and MEK1/2 kinases. ML175 can be used in the research of diseases such as Parkinson's disease.

7-Acetoxy-4-methylcoumarin is an inhibitor of GST.7-Acetoxy-4-methylcoumarin inhibits AFB1-DNA binding in vitro with 36.7% inhibition.

GST-FH.1 is a GST-FH compound, a complex that produces frequent false positive hits (FH) in the interaction between glutathione S-transferase (GST) and glutathione (GSH) . GST-FH.4 inhibits glutathione S-transferase (GST) activity with an IC₅₀ of 0.32 μM.

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.