Gutathione-S-transferase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html Gutathione HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html S-transferaseGlutathione transferases; GSTsGutathione S-transferases (GSTs) are a di

2、verse group of phase II drug metabolizing enzymes whose shared function is theconjugation of glutathione (GSH) to various electrophilic endo- and xenobiotics. GSTs have been implicated in the conjugation ofendogenously produced oxidized metabolites including propenal, 4-hydroxynonenals, organic hydr

3、operoxides, phospholipids, andfatty acid peroxides.On the basis of subcellular localization, the GST enzymes are grouped into three different classes namely, membrane-boundmicrosomal, mitochondrial and cytoplasmic. The leading and most diverse group of GSTs are the cytosolic enzyme spresent inhumans

4、. 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 (),delta(), phi () and tau () are also pres

5、ent in bacteria, insects and plants.GSTs have emerged as a promising therapeutic target because specific isozymes are overexpressed in a wide variety of tumors andmay play a role in the etiology of other diseases, including neurodegenerative diseases, multiple sclerosis, and asthma.www.MedChemE 1 HY

6、PERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html Gutathione HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html S-transferase HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html HYPER

7、LINK https:/www.MedChemE/Targets/Gutathione S-transferase.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html & HYPERLINK https:/www.MedChemE/Targets/Gutathione S-transferase.html HYPERLINK https:/www

8、.MedChemE/Targets/Gutathione S-transferase.html Activators HYPERLINK https:/www.MedChemE/azd9898.html AZD9898 HYPERLINK https:/www.MedChemE/azd9898.html HYPERLINK https:/www.MedChemE/brd2889.html BRD2889Cat. No.: HY-126329 Cat. No.: HY-145413AZD9898 is an orally active leukotriene-C4synthetase (LTC4

9、S, glutathione S-transferase II)inhibitor, with an IC of 0.28 nM. AZD989850mitigates the GABA binding and hepatic toxicitysignal. AZD9898 has the potential to treat asthma.BRD2889 is an analog of the alkaloidpiperlongumine. BRD2889 is a robust modulator ofthe GSTP1-ISCU axis in pulmonary hypertensio

10、n (PH).Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html Coniferyl HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html ferula

11、te HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html HYPERLINK https:/www.MedChemE/curzerene.html CurzereneCat. No.: HY-N1916 Cat. No.: HY-N1963Coniferyl ferulate, a strong inhibitor ofglutathione S-transferase (GST), reversesmultidrug resistance and downregulatesP-glycoprotein. Coniferyl ferula

12、te shows stronginhibition of human placental GST with an IC of500.3M.Curzerene is a sesquiterpene is isolated from therhizome of Curculigo orchioides Gaertn withanti-cancer activity. Curzerene inhibitsglutathione S-transferase A1 (GSTA1) mRNA andprotein expression. Curzerene induces cellapoptosis.Pu

13、rity: 98.56%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 97.0%Clinical Data: No Development ReportedSize: 5 mg (1 mg x 5), 10 mg (1 mg x 10), 1 mg HYPERLINK https:/www.MedChemE/ethacrynic-acid.html Ethacrynic HYPERLINK https:/www.MedChemE/ethacrynic-acid.html HYPERLINK https:

14、/www.MedChemE/ethacrynic-acid.html acid(Etacrynic acid) Cat. No.: HY-B1640 HYPERLINK https:/www.MedChemE/ethacrynic-acid-d5.html Ethacrynic HYPERLINK https:/www.MedChemE/ethacrynic-acid-d5.html HYPERLINK https:/www.MedChemE/ethacrynic-acid-d5.html acid HYPERLINK https:/www.MedChemE/ethacrynic-acid-d

15、5.html HYPERLINK https:/www.MedChemE/ethacrynic-acid-d5.html D5Cat. No.: HY-108538Ethacrynic acid (Etacrynic acid) is a diuretic.Ethacrynic acid is an inhibitor of glutathioneS-transferases (GSTs). Ethacrynic acid is apotent inhibitor of NF-kB-signaling pathway, andalso modulates leukotriene formati

16、on.Ethacrynic acid D5 is a deuterium labeledEthacrynic acid. Ethacrynic acid is a diuretic.Ethacrynic acid is an inhibitor of glutathioneS-transferases (GSTs). Ethacrynic acid is apotent inhibitor of NF-kB-signaling pathway, andalso modulates leukotriene formation.Purity: 99.98%Clinical Data: Launch

17、edSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ezatiostat.html Ezatiostat HYPERLINK https:/www.MedChemE/ezatiostat.html HYPERLINK https:/www.MedChemE/ezatiostat-hydrochloride.html Ezatiostat HYPERLINK https:/www.MedChe

18、mE/ezatiostat-hydrochloride.html HYPERLINK https:/www.MedChemE/ezatiostat-hydrochloride.html hydrochloride(TER199(free base); TLK199) Cat. No.: HY-13634A (TER199; TLK199 hydrochloride) Cat. No.: HY-13634Ezatiostat (TER199 free base; TLK199) is atripeptide analog of glutathione and is aselective and

19、orally active glutathioneS-transferase P1-1 (GSTP1) inhibitor. Ezatiostatleads to JNK activation by inhibiting GSTP1.Ezatiostat hydrochloride (TER199; TLK199hydrochloride) is a tripeptide analog ofglutathione and is a selective and orally activeglutathione S-transferase P1-1 (GSTP1) inhibitor.Ezatio

20、stat hydrochloride leads to JNK activationby inhibiting GSTP1.Purity: 96.0%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/GSTO-IN-2.html GSTO-IN-2 HYPERLINK https:/www.MedChemE/GSTO-IN-2.html HYPERLINK

21、 https:/www.MedChemE/GSTO1-IN-1.html GSTO1-IN-1Cat. No.: HY-112534 Cat. No.: HY-111530GSTO-IN-2 is a glutathione S-transferase inhibitorwith IC s of 3.6, 16.3, and 1.4 M for GSTA2,50GSTM1, and GSTP1-1.GSTO1-IN-1 is a potent glutathione S-transferaseomega 1 (GSTO1) inhibitor with an IC of 31 nM.50Pur

22、ity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/las17.html LAS17 HYPERLINK https:/

23、www.MedChemE/las17.html HYPERLINK https:/www.MedChemE/seneciphylline.html SeneciphyllineCat. No.: HY-115673 Cat. No.: HY-N1282LAS17 is a potent and selective tyrosine-directedirreversible inhibitor forglutathione S-Transferase Pi (GSTP1) . LAS17inhibits GSTP1 activity with an IC of 0.5 M.50Seneciphy

24、lline is a toxic pyrrolizidine alkaloidin Senecio plants. Seneciphylline significantlyincreases the activities of epoxide hydrase andglutathione-S-transferase but causes reduction ofcytochrome P-450 and related monooxygenaseactivities.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 m

25、gPurity: 99.88%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/tk05.html TK05Cat. No.: HY-117143 HYPERLINK https:/www.MedChemE/TLK117.html TLK117(TER117) Cat. No.: HY-13634BTK05 is a potent and selective inhibitor ofleukotriene C4 synthase (LTC4S) with an IC50 of95 nM.TLK117, the