Glutathione-Peroxidase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html Glutathione HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html PeroxidaseGlutathione peroxidases (GPx) are a family of enzymes with the ability to reduc

2、e organic and inorganic hydroperoxides to thecorresponding alcohols using glutathione or thioredoxin as an electron donor. These enzymes promote hydrogen peroxidemetabolism and protect cell membrane structure and function from oxidative damage. Dysregulated GPx expression is connectedwith severe pat

3、hologies, including obesity and diabetes. GPx1 has been reported to be involved in both pro- and anticancer effectsin different tumor models.In mammals, the GPxs family consists of eight members (GPx1-GPx8) identified so far; five of them (GPx1-GPx4 and GPx6) containselenocysteine in the catalytic c

4、enter and the other three are cysteine-containing proteins. GPx1 is one of the most critical membersof the GPxs family that catalytically reduces hydrogen peroxide to produce water. The function of GPx3 is to scavenge H2O2 andlipoperoxides in the plasma to reduce systematic oxidative stress and to m

5、aintain the bioavailability of vascular nitric oxide. Gpx4 isan essential mammalian glutathione peroxidase, which protects cells against detrimental lipid peroxidation and governs a novelform of regulated necrotic cell death, called ferroptosis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Gl

6、utathione Peroxidase.html Glutathione HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html Peroxidase HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html HYPERLINK https:/www.MedChemE/Targets/Glutathione Per

7、oxidase.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html & HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html HYPERLINK https:/www.MedChemE/Targets/Glutathione Peroxidase.html Activators

8、 HYPERLINK https:/www.MedChemE/4-aminobenzohydrazide.html 4-Aminobenzohydrazide(p-Aminobenzohydrazide; p-Aminobenzoic acid hydrazide) Cat. No.: HY-B0880 HYPERLINK https:/www.MedChemE/4-methylesculetin.html 4-MethylesculetinCat. No.: HY-N42884-Aminobenzohydrazide is an irreversible MPOmyeloperoxidase

9、 inhibitor with an IC of 0.3 M.50It is used for the research of subacute stroke.4-Methylesculetin is an orally active naturalcoumarin derivative, with potent anti-oxidant andanti-inflammatory activities. 4-Methylesculetininhibits myeloperoxidase activity and reducesIL-6 level.Purity: 98%Clinical Dat

10、a: No Development ReportedSize: 1 mg, 5 mgPurity: 98.32%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/AZD5904.html AZD5904 HYPERLINK https:/www.MedChemE/AZD5904.html HYPERLINK https:/www.MedChemE/gpx4-in-3.html GPX4-IN-3Cat. No.: HY-111341 Cat. No.: HY-

11、141809AZD5904 is a selective and irreversible inhibitorof human Myeloperoxidase (MPO) with an IC50of 140 nM and has similar potency in mouse andrat.GPX4-IN-3 (26a) is a potent glutathione peroxidase4 (GPX4) inhibitor as a selective ferroptosisinducer. GPX4-IN-3 (26a) exhibits 71.7% inhibitionfor GPX

12、4 with 1 M.Purity: 99.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.69%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/jke-1674.html JKE-1674 HYPERLINK https:/www.MedChemE/jke-1674.ht

13、ml HYPERLINK https:/www.MedChemE/jke-1716.html JKE-1716Cat. No.: HY-138153 Cat. No.: HY-139001JKE-1674 is an orally active glutathioneperoxidase 4 (GPX4) inhibitor and an activemetabolite of GPX4 inhibitor ML-210. JKE-1674, ananalog of ML-210 in which the nitroisoxazole ringis replaced with an -nitr

14、oketoxime. JKE-1674 canconvert into a nitrile oxide JKE-1777.JKE-1716 is a potent and selective nitrolicacid-containing GPX4 inhibitor. JKE-1716 is ableof inducing ferroptosis selectively throughcovalent GPX4 inhibition.Purity: 98.01%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurit

15、y: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mitiperstat.html Mitiperstat HYPERLINK https:/www.MedChemE/mitiperstat.html HYPERLINK https:/www.MedChemE/ml-210.html ML-210Cat. No.: HY-145581 Cat. No.: HY-100003Mitiperstat is the potent inhibitor ofmyeloper

16、oxidase (MPO). Mitiperstat isparticularly useful in the research of prophylaxisof cardiovascular disorders such as heart failureand coronary artery disease related conditions(extracted from patent US20160152623A1).ML-210 is a selective and covalent glutathioneperoxidase 4 (GPX4) inhibitor with an EC

17、 of5030 nM. ML-210 binds the GPX4 selenocysteineresidue. ML-210 has anti-cancer activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/ml162.html ML162 HYPERLINK

18、https:/www.MedChemE/ml162.html HYPERLINK https:/www.MedChemE/mpo-in-1.html MPO-IN-1Cat. No.: HY-100002 Cat. No.: HY-139915ML162 is a covalent glutathione peroxidase 4(GPX4) inhibitor. ML162 has a selective lethaleffect on mutant RAS oncogene-expressing celllines.MPO-IN-1 is a potent, orally active,

19、andirreversible indole-containing inhibitor ofmyeloperoxidase (MPO). MPO-IN-1 has IC s of502.6 M and 5.3 M for MPO and thyroid peroxidase(TPO), respectively. MPO-IN-1 inhibits MPOactivity in an acute mouse model of inflammation.Purity: 99.52%Clinical Data: No Development ReportedSize: 5 mgPurity: 98

20、%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/mpo-in-28.html MPO-IN-28 HYPERLINK https:/www.MedChemE/mpo-in-28.html HYPERLINK https:/www.MedChemE/mpo-in-3.html MPO-IN-3Cat. No.: HY-115486 Cat. No.: HY-1

21、45197MPO-IN-28 (Compound 28) is a myeloperoxidase(MPO) inhibitor with an IC of 44 nM.50MPO-IN-3 is a potent myeloperoxidase (MPO)inhibitor (WO2013068875A1, example 191).Myeloperoxidase (MPO) is a heme-containing enzymebelonging to the peroxidase superfamily.Purity: 98.0%Clinical Data: No Development

22、 ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mpo-in-4.html MPO-IN-4 HYPERLINK https:/www.MedChemE/mpo-in-4.html HYPERLINK https:/www.MedChemE/n-acetyl-lysyltyrosylcysteine-amide.html N-Acetyl HYPERLINK https:/ww

23、w.MedChemE/n-acetyl-lysyltyrosylcysteine-amide.html HYPERLINK https:/www.MedChemE/n-acetyl-lysyltyrosylcysteine-amide.html lysyltyrosylcysteine HYPERLINK https:/www.MedChemE/n-acetyl-lysyltyrosylcysteine-amide.html HYPERLINK https:/www.MedChemE/n-acetyl-lysyltyrosylcysteine-amide.html amideCat. No.:

24、 HY-146651 Cat. No.: HY-125039MPO-IN-4 (compound 12) is a potent and selectivemyeloperoxidase (MPO) inhibitor with anIC 0 of 25 nM. MPO-IN-4 has no effect on methyl50guanine methyl transferase (MGMT).N-Acetyl lysyltyrosylcysteine amide is a potent,reversible, specific, and non-toxic tripeptideinhibi

25、tor of myeloperoxidase (MPO). N-Acetyllysyltyrosylcysteine amide effectively inhibitsMPO generation of toxic oxidants in vivo.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.81%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.

26、MedChemE/nbdhex.html NBDHEX HYPERLINK https:/www.MedChemE/nbdhex.html HYPERLINK https:/www.MedChemE/PF-06282999.html PF-06282999Cat. No.: HY-135318 Cat. No.: HY-19321NBDHEX is a potent glutathione S-transferase P1-1(GSTP1-1) inhibitor. NBDHEX induces apoptosis oftumor cells.PF-06282999 is a potent a

27、nd selectivemyeloperoxidase inhibitor which is potentialuseful for the treatment of cardiovasculardiseases.Purity: 98.58%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.41%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK

28、 https:/www.MedChemE/PF-1355.html PF-1355 HYPERLINK https:/www.MedChemE/PF-1355.html HYPERLINK https:/www.MedChemE/pkumdl-lc-101-d04.html PKUMDL-LC-101-D04(PF-06281355) Cat. No.: HY-100873 (GPX4-Activator-1d4) Cat. No.: HY-115627PF-1355 is a selective 2-thiouracilmechanism-based MPO inhibitor, used

29、for treatmentof vasculitic diseases.PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a potentferroptosis regulator glutathione peroxidase 4(GPX4) allosteric activator (pEC =4.7).50PKUMDL-LC-101-D04 increases GPX4 activity to 150%at 20 M in the cell-free assay and 61 M in cellextracts.Purity: 99.86%Clinical

30、 Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/RSL3-1S,3R-.html RSL3 HYPERLINK https:/www.MedChemE/RSL3-1S,3R-.html HYPERLINK https:/www.MedChemE/Tinoridine_hydrochloride.html Tinoridine HYPERLINK https:/www.MedChemE/Tinoridine_hydrochloride.html HYPERLINK https:/www.MedChemE/Tinoridine_hydrochloride.html hydrochloride(1S,3R)-RSL3) Cat. No.: HY-100218A (Y-3642 hydrochloride) Cat. No.: HY-111354RSL3 (1