Keap1-Nrf2-Activators-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html Keap1-Nrf2Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS). Keap1 isan E3 ligase, which induces the degradation of Nrf2 by ubiquitin-proteasome system (UPS). Upregulation o

2、f Nrf2 inducing byinactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation andmetabolism. For this case, Nrf2 is an attractive molecule as a therapeutic target in cancer and a lot number of Nrf2 inhibitors aredeveloped. Whats inte

3、resting, Nrf2 induction is also reported to be treatment strategies for accelerating the detoxification ofcarcinogens and protect the body from chemical carcinogenesis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html Keap1-Nrf2 HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.htm

4、l HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html Agonists HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html & HYPER

5、LINK https:/www.MedChemE/Targets/Keap1-Nrf2.html HYPERLINK https:/www.MedChemE/Targets/Keap1-Nrf2.html Activators HYPERLINK https:/www.MedChemE/_addition_-DHMEQ.html (+)-DHMEQ HYPERLINK https:/www.MedChemE/_addition_-DHMEQ.html (1R,2R,6R)-Dehydroxymethylepoxyquinomicin;(1R,2R,6R)-DHMEQ) Cat. No.: HY

6、-14645A HYPERLINK https:/www.MedChemE/_E_-6-Dehydroparadol.html (E)-6-DehydroparadolCat. No.: HY-77293(+)-DHMEQ is an activator of antioxidanttranscription factor Nrf2. (+)-DHMEQ is theenantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kBthan its enantiomer (+)-DHMEQ.(E)-Dehydroparadol, an oxidative met

7、abolite of-Shogaol (HY-14616), is a potent Nrf2 activator.(E)-Dehydroparadol can inhibit the growth andinduce the apoptosis of human cancer cells.Purity: 99.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mgPurity: 95.0%Clinical Data: No Development ReportedSize: 10

8、mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/4-Hydroxyphenylacetic_acid.html 4-Hydroxyphenylacetic HYPERLINK https:/www.MedChemE/4-Hydroxyphenylacetic_acid.html HYPERLINK https:/www.MedChemE/4-Hydroxyphenylacetic_acid.html acid HYPERLINK https:/www.MedChemE/4-Hydroxyphen

9、ylacetic_acid.html HYPERLINK https:/www.MedChemE/4-hydroxyphenylacetic-acid-d6.html 4-Hydroxyphenylacetic HYPERLINK https:/www.MedChemE/4-hydroxyphenylacetic-acid-d6.html HYPERLINK https:/www.MedChemE/4-hydroxyphenylacetic-acid-d6.html acid-d6Cat. No.: HY-N1902 Cat. No.: HY-N1902S4-hydroxyphenylacet

10、ic acid, a majormicrobiota-derived metabolite of polyphenols, isinvolved in the antioxidative action.4-hydroxyphenylacetic acid induces expression ofNrf2.4-Hydroxyphenylacetic acid-d6 is the deuteriumlabeled 4-Hydroxyphenylacetic acid.4-hydroxyphenylacetic acid, a majormicrobiota-derived metabolite

11、of polyphenols, isinvolved in the antioxidative action.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/4-Octyl_Itaconate.html 4-Octyl HYPERLINK https:/www.MedChemE/4-Octyl_Itaco

12、nate.html HYPERLINK https:/www.MedChemE/4-Octyl_Itaconate.html Itaconate HYPERLINK https:/www.MedChemE/4-Octyl_Itaconate.html HYPERLINK https:/www.MedChemE/5-7-dihydroxychromone.html 5,7-DihydroxychromoneCat. No.: HY-112675 Cat. No.: HY-N19704-Octyl Itaconate is a cell-permeable Itaconatederivative.

13、 Itaconate is an anti-inflammatorymetabolite that activates Nrf2 via alkylation ofKEAP1.5,7-Dihydroxychromone, the extract of Cudraniatricuspidata, activates Nrf2/ARE signal and exertsneuroprotective effects against 6-hydroxydopamine(6-OHDA)-induced oxidative stress and apoptosis.Purity: 99.98%Clini

14、cal Data: No Development ReportedSize: 10 mM 1 mL, 50 mg, 100 mg, 200 mg, 500 mgPurity: 99.98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/aem1.html AEM1 HYPERLINK https:/www.MedChemE/aem1.html HYPERLINK https:/www.MedChemE/antroquinonol.html AntroquinonolCat

15、. No.: HY-113848(+)-Antroquinonol) Cat. No.: HY-19893AEM1 is a Nrf2 inhibitor. AEM1 reduces theexpressions of Nrf2-dependent genes in A549 cellsand inhibits the growth of A549 cells in vitro andin vivo.Antroquinonol (+)-Antroquinonol), a ubiquinonederivative from the mushroom Antrodiacamphorata, has

16、 hepatoprotective,anti-inflammatory, and anti-cancer effects.Antroquinonol can be used for the research ofcolon cancer.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Astilbin.html Astilb

17、in HYPERLINK https:/www.MedChemE/Astilbin.html HYPERLINK https:/www.MedChemE/Bardoxolone.html BardoxoloneCat. No.: HY-N0509(CDDO; RTA 401) Cat. No.: HY-14909Astilbin is a flavonoid compound and enhancesNRF2 activation. Astilbin also suppresses TNF-expression and NF-B activation.Bardoxolone is a nove

18、l nuclear regulator factor(Nrf-2) activator.Purity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.14%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www

19、.MedChemE/Bardoxolone-methyl.html Bardoxolone HYPERLINK https:/www.MedChemE/Bardoxolone-methyl.html HYPERLINK https:/www.MedChemE/Bardoxolone-methyl.html methyl(RTA 402; NSC 713200; CDDO Methyl ester) Cat. No.: HY-13324 HYPERLINK https:/www.MedChemE/Brusatol.html Brusatol(NSC 172924) Cat. No.: HY-19

20、543Bardoxolone methyl (NSC 713200; RTA 402; CDDOMethyl ester) is a synthetic triterpenoid compoundwith potential antineoplastic andanti-inflammatory activities, acting as anactivator of the Nrf2 pathway and an inhibitor ofthe NF-B pathway.Brusatol (NSC 172924) is a unique inhibitorof the Nrf2 pathwa

21、y that sensitizes a broadspectrum of cancer cells to Cisplatin and otherchemotherapeutic agents. Brusatol enhances theefficacy of chemotherapy by inhibiting theNrf2-mediated defense mechanism.Purity: 99.72%Clinical Data: Phase 3Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mgPurity: 99.89%Clin

22、ical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Carnosol.html Carnosol HYPERLINK https:/www.MedChemE/Carnosol.html HYPERLINK https:/www.MedChemE/cbr-470-1.html CBR-470-1Cat. No.: HY-N0643 Cat. No.: HY-134205ACarnosol is a potent Ribosomal S6 Kinase (RSK2

23、)inhibitor that could be useful for treatinggastric cancer, with an IC of 5.5 M. Carnosol,50a Nrf2 activator, increases the nuclear levels ofNrf2 and can promote the expression of hemeoxygenase 1 (HMOX1).CBR-470-1 is an inhibitor of the glycolytic enzymephosphoglycerate kinase 1 (PGK1). CBR-470-1 is

24、also a non-covalent Nrf2 activator. CBR-470-1protects SH-SY5Y neuronal cells againstMPP+-induced cytotoxicity through activation ofthe Keap1-Nrf2 cascade.Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98.35%Clinical Data: No Development ReportedSize:

25、10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cbr-470-2.html CBR-470-2Cat. No.: HY-134001 HYPERLINK https:/www.MedChemE/cddo-dhtfea.html CDDO-dhTFEA(RTA dh404) Cat. No.: HY-112671CBR-470-2, a glycine-substituted analog, canactivate NRF2 signaling. CBR-470-2 can be usedf

26、or the research of modulation glycolysis.CDDO-dhTFEA (RTA dh404) is a synthetic oleananetriterpenoid compound which potently activatesNrf2 and inhibits the pro-inflammatorytranscription factor NF-B.Purity: 99.22%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.

27、71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CDDO-EA.html CDDO-EA HYPERLINK https:/www.MedChemE/CDDO-EA.html HYPERLINK https:/www.MedChemE/CDDO-Im.html CDDO-Im(CDDO ethyl amide; TP319; RTA 405) Cat. No.: HY-12213 (RTA-403;

28、 TP-235; CDDO-Imidazolide) Cat. No.: HY-15725CDDO-EA is an NF-E2 related factor 2/antioxidantresponse element (Nrf2/ARE) activator.CDDO-Im (RTA-403) is an activator of Nrf2 andPPAR, with Ks of 232 and 344 nM for PPAR andiPPAR.Purity: 98.46%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg

29、, 10 mg, 50 mg, 100 mgPurity: 98.19%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/chaetominine.html Chaetominine HYPERLINK https:/www.MedChemE/chaetominine.html HYPERLINK https:/www.MedChemE/corynoline.html Corynoline(-)-Chaetominine) Cat. No.: HY-

30、125136Cat. No.: HY-N0826Chaetominine is an alkaloidal metabolite.Chaetominine has cytotoxicity against humanleukemia K562 and colon cancer SW1116 cell lines.Chaetominine reduces MRP1-mediated drug resistancevia inhibiting PI3K/Akt/Nrf2 signaling pathway inK562/Adr human leukemia cells.Corynoline is

31、a reversible and noncompetitiveacetylcholinesterase (AChE) inhibitor with anIC of 30.6 M. Corynoline exhibits50anti-inflammatory activity by activating Nrf2.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.06%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

32、 mg, 20 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Curcumin.html Curcumin(Diferuloylmethane; Natural Yellow 3; Turmeric yellow) Cat. No.: HY-N0005 HYPERLINK https:/www.MedChemE/curcumin-d6.html Curcumin-d6 HYPERLINK https:/www.MedChemE/curcumin-d6.html (Diferuloylmethane-d6; Natural Yellow 3-d6;

33、Turmeric yellow-d6) Cat. No.: HY-N0005SCurcumin (Diferuloylmethane), a natural phenoliccompound, is a p300/CREB-binding protein-specificinhibitor of acetyltransferase, represses theacetylation of histone/nonhistone proteins andhistone acetyltransferase-dependent chromatintranscription.Curcumin D6 (D

34、iferuloylmethane D6) is a deuteriumlabeled Curcumin (Turmeric yellow). Curcumin(Turmeric yellow) is a natural phenolic compoundwith diverse pharmacologic effects includinganti-inflammatory, antioxidant, antiproliferativeand antiangiogenic activities.Purity: 96.0%Clinical Data: Phase 4Size: 10 mM 1 m

35、L, 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Danshensu.html Danshensu(Dan shen suan A; Salvianic acid A) Cat. No.: HY-N1913 HYPERLINK https:/www.MedChemE/ddo-7263.html DDO-7263Cat. No.: HY-144634Danshensu, an active ingredien

36、t of Salviamiltiorrhiza, shows wide cardiovascular benefitby activating Nrf2 signaling pathway.DDO-7263, a 1,2,4-Oxadiazole derivative, is apotent Nrf2 activator. DDO-7263 upregulates Nrf2through binding to Rpn6 to block the assembly of26S proteasome and the subsequent degradation ofubiquitinated Nr

37、f2.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dehydrocurdione.html Dehydrocurdione HYPERLINK https:/www.MedChemE/dehydrocurdione.html HYPERLINK https:/www.Med

38、ChemE/desfluoro-ezetimibe.html Desfluoro-ezetimibeCat. No.: HY-N8160 Cat. No.: HY-136059Dehydrocurdione, a zedoary-derived sesquiterpene,induces heme oxygenase (HO)-1, an antioxidativeenzyme, in RAW 264.7 macrophages. Dehydrocurdioneinteracts with Keap1, resulting in Nrf2translocation followed by ac

39、tivation of the HO-1E2 enhancer.Desfluoro-ezetimibe is a desfluoro impurity ofEzetimibe. Ezetimibe is a potent, metabolicallystable cholesterol absorption inhibitor. Ezetimibeis a Niemann-Pick C1-like1 (NPC1L1) inhibitor,and is a potent Nrf2 activator.Purity: 98%Clinical Data: No Development Reporte

40、dSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dibenzoylmethane.html Dibenzoylmethane HYPERLINK https:/www.MedChemE/dibenzoylmethane.html HYPERLINK https:/www.MedChemE/Dimethyl-fumarate.html Dimethyl HYPERLINK https:/www.MedCh

41、emE/Dimethyl-fumarate.html HYPERLINK https:/www.MedChemE/Dimethyl-fumarate.html fumarateCat. No.: HY-W009731 Cat. No.: HY-17363Dibenzoylmethane, a minor ingredient in licorice,activates Nrf2 and prevents various cancers andoxidative damage. Dibenzoylmethane, an analog ofcurcumin, results in dissocia

42、tion from Keap1 andnuclear translocation of Nrf2.Dimethyl fumarate (DMF) is an orally active andbrain-penetrant Nrf2 activator and inducesupregulation of antioxidant gene expression.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 500 mgPurity: 99.88%Clinical Data: LaunchedSize:

43、10 mM 1 mL, 500 mg, 5 g HYPERLINK https:/www.MedChemE/dimethyl-fumarate-d6.html Dimethyl HYPERLINK https:/www.MedChemE/dimethyl-fumarate-d6.html HYPERLINK https:/www.MedChemE/dimethyl-fumarate-d6.html fumarate-d6 HYPERLINK https:/www.MedChemE/dimethyl-fumarate-d6.html HYPERLINK https:/www.MedChemE/E

44、riodictyol.html EriodictyolCat. No.: HY-17363S(Huazhongilexone) Cat. No.: HY-N0637Dimethyl fumarate D6 is a deuterium labeledDimethyl fumarate. Dimethyl fumarate is a nuclearfactor (erythroid-derived)-like 2 (Nrf2) pathwayactivator and induces upregulation of antioxidantgene expression.Eriodictyol i

45、s a flavonoid isolated from theChinese herb, with antioxidant andanti-inflammatory activity. Eriodictyol inducesNrf2 signaling pathway. Eriodictyol is also apotent influenza RNA-dependent RNA polymeraseinhibitor with an IC of 18 nM.50Purity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 m

46、g, 10 mgPurity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/eriodictyol-7-o-glucoside.html Eriodictyol-7-O-glucoside(Eriodictyol 7-O-D-glucoside) Cat. No.: HY-N3847 HYPERLINK https:/www.Med

47、ChemE/Ezetimibe.html Ezetimibe(SCH 58235) Cat. No.: HY-17376Eriodictyol-7-O-glucoside (Eriodictyol7-O-D-glucoside), a flavonoid, is a potent freeradical scavenger. Eriodictyol-7-O-glucoside isalso an Nrf2 activator, confers protectionagainst Cisplatin-induced toxicity.Ezetimibe (SCH 58235) is a pote

48、nt cholesterolabsorption inhibitor. Ezetimibe is a Niemann-PickC1-like1 (NPC1L1) inhibitor, and is a potentNrf2 activator.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK htt

49、ps:/www.MedChemE/ezetimibe-ketone.html Ezetimibe HYPERLINK https:/www.MedChemE/ezetimibe-ketone.html HYPERLINK https:/www.MedChemE/ezetimibe-ketone.html ketone(EZM-K) Cat. No.: HY-133114 HYPERLINK https:/www.MedChemE/ezetimibe-d4-diacetate.html Ezetimibe-d4 HYPERLINK https:/www.MedChemE/ezetimibe-d4

50、-diacetate.html HYPERLINK https:/www.MedChemE/ezetimibe-d4-diacetate.html diacetateCat. No.: HY-17376S2Ezetimibe ketone (EZM-K) is a phase-I metaboliteof Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1(NPC1L1) inhibitor, and is a potent Nrf2activator. Ezetimibe is a potent cholesterolabsorption inhi

51、bitor.Ezetimibe-d4 diacetate is the deuterium labeledEzetimibe. Ezetimibe (SCH 58235) is a potentcholesterol absorption inhibitor. Ezetimibe is aNiemann-Pick C1-like1 (NPC1L1) inhibitor, and isa potent Nrf2 activator.Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data

52、: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/ezetimibe-d4-1.html Ezetimibe-d4-1(SCH 58235-d4-1) Cat. No.: HY-17376S1 HYPERLINK https:/www.MedChemE/garcinone-d.html Garcinone HYPERLINK https:/www.MedChemE/garcinone-d.html HYPERLINK https:/www.MedChemE/garcinone-d.html DCat

53、. No.: HY-N6953Ezetimibe-d4 is deuterium labeled Ezetimibe.Ezetimibe (SCH 58235) is a potent cholesterolabsorption inhibitor. Ezetimibe is a Niemann-PickC1-like1 (NPC1L1) inhibitor, and is a potent Nrf2activator.Garcinone D, a natural xanthone from mangosteen,promotes the proliferation of C17.2 neur

54、al stemcell.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.19%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Ginsenoside-Rh3.html Ginsenoside HYPERLINK https:/www.MedChemE/Ginsenoside-Rh3.html HYPERLINK https:/www.

55、MedChemE/Ginsenoside-Rh3.html Rh3 HYPERLINK https:/www.MedChemE/Ginsenoside-Rh3.html HYPERLINK https:/www.MedChemE/Hesperin.html HesperinCat. No.: HY-N0606 Cat. No.: HY-101371Ginsenoside Rh3 is a bacterial metabolite ofGinsenoside Rg5. Ginsenoside Rh3 treatment inhuman retinal cells induces Nrf2 act

56、ivation.Hesperin is a bioactive ingredient present inJapanese horseradish (wasabi) and has been shownto be an Nrf2 activator.Purity: 99.95%Clinical Data: No Development ReportedSize: 5 mgPurity: 98.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:

57、/www.MedChemE/Hinokitiol.html Hinokitiol HYPERLINK https:/www.MedChemE/Hinokitiol.html HYPERLINK https:/www.MedChemE/k67.html K67(-Thujaplicin) Cat. No.: HY-B2230Cat. No.: HY-111126Hinokitiol is a component of essential oilsisolated from Chymacyparis obtusa, reduces Nrf2expression, and decreases DNM

58、T1 and UHRF1 mRNAand protein expression, with anti-infective,anti-oxidative, and anti-tumor activities.K67 specifically inhibits the interaction betweenKeap1 and S -phosphorylated p62. K67 prevents349p-p62 from blocking the binding of Keap1 and Nrf2.Purity: 98.24%Clinical Data: No Development Report

59、edSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/keap1-nrf2-in-1.html Keap1-Nrf2-IN-1 HYPERLINK https:/www.MedChemE/keap1-nrf2-in-1.html HYPERLINK https:/www.MedChemE/keap1-nrf2-in-1-tfa.html Keap1-Nrf2-IN-

60、1 HYPERLINK https:/www.MedChemE/keap1-nrf2-in-1-tfa.html HYPERLINK https:/www.MedChemE/keap1-nrf2-in-1-tfa.html TFACat. No.: HY-126245 Cat. No.: HY-126245AKeap1-Nrf2-IN-1 is a Keap1 (Kelch-likeECH-associated protein 1)-Nrf2 (nuclear factorerythroid 2-related factor 2) protein-proteininteraction inhi