STAT-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/STAT.html STATSTAT is a family of cytoplasmic protein that regulates many aspects of growth, survival and differentiation in cells. The transcriptionfactors of this family are activated by Janus kinase and dysregulation of this pathway is frequently observed in

2、 primary tumours andleads to increased angiogenesis, enhanced survival of tumours and immunosuppression. Gene knockout studies have providedevidence that STAT proteins are involved in the development and function of the immune system and play a role in maintainingimmune tolerance and tumour surveill

3、ance. STAT proteins were originally described as latent cytoplasmic transcription factors thatrequire phosphorylation for nuclear retention. The unphosphorylated STAT proteins shuttle between cytosol and the nucleuswaiting for its activation signal. Once the activated transcription factor reaches th

4、e nucleus, it binds to consensus DNA-recognitionmotif called gamma-activated sites (GAS) in the promoter region of cytokine-inducible genes and activates transcription of thesegenes.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/STAT.html STAT HYPERLINK https:/www.MedChemE/Targets/STAT.html HY

5、PERLINK https:/www.MedChemE/Targets/STAT.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/STAT.html HYPERLINK https:/www.MedChemE/Targets/STAT.html Activators, HYPERLINK https:/www.MedChemE/Targets/STAT.html HYPERLINK https:/www.MedChemE/Targets/STAT.html Agonists HYPERLINK https:/www.MedChemE

6、/Targets/STAT.html HYPERLINK https:/www.MedChemE/Targets/STAT.html & HYPERLINK https:/www.MedChemE/Targets/STAT.html HYPERLINK https:/www.MedChemE/Targets/STAT.html Antagonists HYPERLINK https:/www.MedChemE/plus-ochromycinone.html (+)-Ochromycinone(STA-21) Cat. No.: HY-121482 HYPERLINK https:/www.Me

7、dChemE/e-z-ag490.html (E/Z)-AG490(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42) Cat. No.: HY-107459(+)-Ochromycinone is a natural antibiotic thatpotently inhibits STAT3. (+)-Ochromycinone is usedin the researches of cancers and psoriasis.(E/Z)-AG490 (E/Z)-Tyrphostin AG490) is a racemiccompound of (E)

8、-AG490 and (Z)-AG490 isomers.(E)-AG490 (HY-12000) is a tyrosine kinase inhibitorthat inhibits EGFR, Stat-3 and JAK2/3.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 96.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/r-lisofylline.html

9、(R)-Lisofylline(R)-Lisophylline) Cat. No.: HY-109854A HYPERLINK https:/www.MedChemE/stat3-in-7.html 1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy) HYPERLINK https:/www.MedChemE/stat3-in-7.html phenyl)urea HYPERLINK https:/www.MedChemE/stat3-in-7.html Cat. No.: HY-136658(R)-Lisofylline

10、(R)-Lisophylline) is a(R)-enantiomer of the metabolite of Pentoxifyllinewith anti-inflammatory properties.STAT3-IN-7 is a Sorafenib analogue and potentlyinhibits the phosphorylation of STAT3. STAT3-IN-7induces cell apoptosis through SHP-1 dependentSTAT3 inactivation. STAT3-IN-7 does not inhibitkinas

11、e activity and has anticancer effects.Purity: 97.0%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/2-np.html 2-NPCat. No.: HY-W013523 HYPERLINK https:/www.MedChemE/5-15-diphenylporphyrin.html 5,15-Dipheny

12、lporphyrin(5,15-DPP) Cat. No.: HY-W0351372-NP is a selective enhancer of STAT1transcription. 2-NP can enhance the ability ofIFN- to inhibit the proliferation of human breastcancer and fibrosarcoma cells.5,15-Diphenylporphyrin (5,15-DPP) is a selectiveSTAT3-SH2 antagonist (IC s of 0.28 M and 10 M50fo

13、r STAT3 and STAT1, respectively).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/ac-4-130.html AC-4-130 HYPERLINK https:/www.MedChemE/ac-4-130.html HYPERLINK https:/www.MedChemE/act001.ht

14、ml ACT001Cat. No.: HY-124500 Cat. No.: HY-128861AAC-4-130 is a potent STAT5 SH2 domain inhibitor.AC-4-130 directly binds to STAT5 and disruptsSTAT5 activation, dimerization, nucleartranslocation, and STAT5-dependent genetranscription.ACT001 is an orally active PAI-1 inhibitor byinhibiting the phosph

15、orylation of PI3K and AKT.ACT001 inhibits the phosphorylation of STAT3 andPD-L1 expression by directly binding to STAT3.Purity: 99.87%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.62%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg,

16、 50 mg HYPERLINK https:/www.MedChemE/AG-490.html AG490 HYPERLINK https:/www.MedChemE/AG-490.html HYPERLINK https:/www.MedChemE/Alantolactone.html Alantolactone(Tyrphostin AG490; Tyrphostin B42) Cat. No.: HY-12000 (+)-Alantolactone; Alant camphor; Inula camphor) Cat. No.: HY-N0038AG490 (Tyrphostin AG

17、490) is a tyrosine kinaseinhibitor that inhibits EGFR, Stat-3 andJAK2/3.Alantolactone is a selective STAT3 inhibitor,with potent anticancer activity. Alantolactoneinduces apoptosis in cancer.Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.

18、94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/angoline.html Angoline HYPERLINK https:/www.MedChemE/angoline.html HYPERLINK https:/www.MedChemE/angoline-hydrochloride

19、.html Angoline HYPERLINK https:/www.MedChemE/angoline-hydrochloride.html HYPERLINK https:/www.MedChemE/angoline-hydrochloride.html hydrochlorideCat. No.: HY-N7674 Cat. No.: HY-N7674AAngoline is a potent and selective IL6/STAT3signaling pathway inhibitor with an IC of5011.56 M. Angoline inhibits STAT

20、3 phosphorylationand its target gene expression, and inhibitscancer cell proliferation.Angoline hydrochloride is a potent and selectiveIL6/STAT3 signaling pathway inhibitor with anIC of 11.56 M. Angoline hydrochloride inhibits50STAT3 phosphorylation and its target geneexpression, and inhibits cancer

21、 cellproliferation.Purity: 99.67%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/aptstat3-9r.html APTSTAT3-9R HYPERLINK https:/www.MedChemE/aptstat3-9r.html HYPERLINK https:/www.MedChemE/arnicolide-d.html Arnic

22、olide HYPERLINK https:/www.MedChemE/arnicolide-d.html HYPERLINK https:/www.MedChemE/arnicolide-d.html DCat. No.: HY-P2282 Cat. No.: HY-N6843APTSTAT3-9R, a specific STAT3-binding peptide,inhibits STAT3 activation and downstream signalingby specifically blocking STAT3 phosphorylation.APTSTAT3-9R exert

23、s antiproliferative effects andantitumor activity.Arnicolide D is a sesquiterpene lactone isolatedfrom Centipeda minima. Arnicolide D modulatesthe cell cycle, activates the caspase signalingpathway and inhibits the PI3K/AKT/mTOR andSTAT3 signaling pathways.Purity: 98%Clinical Data: No Development Re

24、portedSize: 1 mg, 5 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Artesunate.html Artesunate HYPERLINK https:/www.MedChemE/Artesunate.html HYPERLINK https:/www.MedChemE/artesunate-d3.html Artesunate-d3Cat. No.: HY-N0193 Cat. No.: HY-N0193SArtesu

25、nate is an inhibitor of both STAT-3 andexported protein 1 (EXP1).Artesunate-d3 is the deuterium labeled Artesunate.Artesunate is an inhibitor of both STAT-3 andexported protein 1 (EXP1).Purity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data: No Development Report

26、edSize: 10 mg HYPERLINK https:/www.MedChemE/artesunate-d4.html Artesunate-d4 HYPERLINK https:/www.MedChemE/artesunate-d4.html HYPERLINK https:/www.MedChemE/AS1517499.html AS1517499Cat. No.: HY-N0193S1 Cat. No.: HY-100614Artesunate-d4 is deuterium labeled Artesunate.Artesunate is an inhibitor of both

27、 STAT-3 andexported protein 1 (EXP1).AS1517499 is a potent and brain-permeable STAT6phosphorylation inhibitor with an IC of 21 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

28、 HYPERLINK https:/www.MedChemE/as1810722.html AS1810722 HYPERLINK https:/www.MedChemE/as1810722.html HYPERLINK https:/www.MedChemE/as2863619.html AS2863619Cat. No.: HY-134772 Cat. No.: HY-126675AAS1810722 is an orally active and potent STAT6inhibitor with an IC of 1.9 nM. AS1810722 shows50a good pro

29、file of CYP3A4 inhibition. AS1810722, aderivative of fused bicyclic pyrimidine, has thepotential for allergic diseases such as asthma andatopic diseases research.AS2863619 enables conversion of antigen-specificeffector/memory T cells into Foxp3+ regulatory T(T ) cells for the treatment of variousreg

30、immunological diseases.Purity: 98.56%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/as2863619-free-base.html AS2863619

31、 HYPERLINK https:/www.MedChemE/as2863619-free-base.html HYPERLINK https:/www.MedChemE/as2863619-free-base.html free HYPERLINK https:/www.MedChemE/as2863619-free-base.html HYPERLINK https:/www.MedChemE/as2863619-free-base.html baseCat. No.: HY-126675 HYPERLINK https:/www.MedChemE/ascochlorin.html Asc

32、ochlorin(Ilicicolin D) Cat. No.: HY-101021AS2863619 free base enables conversion ofantigen-specific effector/memory T cells intoFoxp3+ regulatory T (T ) cells for theregtreatment of various immunological diseases.Ascochlorin (Ilicicolin D), an isoprenoidantibiotic, mediates its anti-tumor effectspre

33、dominantly through the suppression of STAT3signaling cascade. Ascochlorin induces apoptosis.Anti-inflammatory activity.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 500 g, 1 mg HYPERLINK https:/ww

34、w.MedChemE/Atractylenolide-I.html Atractylenolide HYPERLINK https:/www.MedChemE/Atractylenolide-I.html HYPERLINK https:/www.MedChemE/Atractylenolide-I.html I HYPERLINK https:/www.MedChemE/Atractylenolide-I.html HYPERLINK https:/www.MedChemE/Balsalazide.html BalsalazideCat. No.: HY-N0201 Cat. No.: HY

35、-B0667Atractylenolide I is a sesquiterpene derived fromthe rhizome of Atractylodes macrocephala,possesses diverse bioactivities, such asneuroprotective, anti-allergic, anti-inflammatoryand anticancer properties.Balsalazide could suppress colitis-associatedcarcinogenesis through modulation of IL-6/ST

36、AT3pathway.Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.20%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Balsalazide-sodium-hydrate.html Balsalazide HYPERLINK https:/www.MedChemE/Balsalazide-sodium-hy

37、drate.html HYPERLINK https:/www.MedChemE/Balsalazide-sodium-hydrate.html sodium HYPERLINK https:/www.MedChemE/Balsalazide-sodium-hydrate.html HYPERLINK https:/www.MedChemE/Balsalazide-sodium-hydrate.html hydrate(Balsalazide disodium dihydrate) Cat. No.: HY-B0667A HYPERLINK https:/www.MedChemE/balsal

38、azide-d4.html Balsalazide-d4Cat. No.: HY-B0667S1Balsalazide sodium hydrate could suppresscolitis-associated carcinogenesis throughmodulation of IL-6/STAT3 pathway.Balsalazide-d4 is deuterium labeled Balsalazide.Balsalazide could suppress colitis-associatedcarcinogenesis through modulation of IL-6/ST

39、AT3pathway.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bd750.html BD750 HYPERLINK https:/www.MedChemE/bd750.html HYPERLINK https:/www.MedChemE/BP-1-102.html BP-1-102Cat. No.: HY-131140 Cat. No.: HY-

40、100493BD750, an effective immunosuppressant and aJAK3/STAT5 inhibitor, inhibits IL-2-inducedJAK3/STAT5-dependent T cell proliferation, withIC values of 1.5 M and 1.1 M in mouse and human50T cells, respectively.BP-1-102 is an orally available, small-moleculeinhibitor of transcription factor Stat3, wi

41、th anIC of 6.8 M.50Purity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/brevilin-a.html Brevilin HYPERLINK https:/www.MedChemE/brev

42、ilin-a.html HYPERLINK https:/www.MedChemE/brevilin-a.html A HYPERLINK https:/www.MedChemE/brevilin-a.html HYPERLINK https:/www.MedChemE/c188.html C188Cat. No.: HY-N2959(CPD188) Cat. No.: HY-112338Brevilin A is a sesquiterpene lactone isolatedfrom Centipeda minima with anti-tumor activity.Brevilin A

43、is a selective inhibitor of JAK-STATsignal pathway by attenuating the JAKs activityand blocking STAT3 signaling (IC =10.6 M) in50Cancer Cells.C188 is a STAT3 inhibitor that inhibitsIL-6-stimulated STAT3 phosphorylation and nucleartranslocation in HepG2 cells by targeting STAT3SH2 domain peptide-bind

44、ing pocket.Purity: 99.77%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/C188-9.html C188-9(TTI-101) Cat. No.: HY-112288 HYPERLINK https:/w

45、ww.MedChemE/Casticin.html Casticin(Vitexicarpin) Cat. No.: HY-N0516C188-9 (TTI-101) is a STAT3 inhibitor, with aK of 4.7 nM. C188-9 inhibits G-CSF-induceddSTAT3 activation and STAT3-dependent geneexpression. C188-9 induces apoptosis in AML celllines and primary samples and inhibits colonyformation b

46、y primary AML blasts.Casticin is a methyoxylated flavonol isolated fromViticis Fructus, with antimitotic andanti-inflammatory effect. Casticin inhibits theactivation of STAT3.Purity: 99.90%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.67%Clinical Data: No Develo

47、pment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/cenisertib.html Cenisertib(AS-703569; R-763) Cat. No.: HY-13072 HYPERLINK https:/www.MedChemE/cirsilineol.html CirsilineolCat. No.: HY-119347Cenisertib (AS-703569) is an ATP-competitivemulti-kinase inhibitor that blocks

48、 the activity ofAurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.Cirsilineol, a natural flavone compound,selectively inhibits IFN-/STAT1/T-bet signalingin intestinal CD4+ T cells. Cirsilineol haspotent immunosuppressive and anti-tumorproperties.Purity: 99.64%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg,

49、 10 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CMD178.html CMD178 HYPERLINK https:/www.MedChemE/CMD178.html HYPERLINK https:/www.MedChemE/cmd178-tfa.html CMD178 HYPERLINK https:/www.MedChemE/cmd178-tfa.html HYPERLINK https:/www.

50、MedChemE/cmd178-tfa.html TFACat. No.: HY-P1453 Cat. No.: HY-P1453ACMD178 is a lead peptide that consistently reducedthe expression of Foxp3 and STAT5 induced byIL-2/s IL-2R signaling. CMD178 also is aninhibitor of STAT5 and inhibit T cellregdevelopment.CMD178 (TFA) is a lead peptide that consistentl

51、yreduces the expression of Foxp3 and STAT5 inducedby IL-2/s IL-2R signaling. CMD178 (TFA) also isan inhibitor of STAT5 and inhibits T cellsregdevelopment.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg,

52、 10 mg HYPERLINK https:/www.MedChemE/Colivelin.html Colivelin HYPERLINK https:/www.MedChemE/Colivelin.html HYPERLINK https:/www.MedChemE/Colivelin_TFA.html Colivelin HYPERLINK https:/www.MedChemE/Colivelin_TFA.html HYPERLINK https:/www.MedChemE/Colivelin_TFA.html TFACat. No.: HY-P1061 Cat. No.: HY-P

53、1061AColivelin is a brain penetrant neuroprotectivepeptide and a potent activator of STAT3,suppresses neuronal death by activatingSTAT3 in vitro.Colivelin TFA is a brain penetrant neuroprotectivepeptide and a potent activator of STAT3,suppresses neuronal death by activatingSTAT3 in vitro.Purity: 98%

54、Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.22%Clinical Data: No Development ReportedSize: 500 g, 1 mg HYPERLINK https:/www.MedChemE/Corylifol-A.html Corylifol HYPERLINK https:/www.MedChemE/Corylifol-A.html HYPERLINK https:/www.MedChemE/Corylifol-A.html A HYPERLINK https:/www.Me

55、dChemE/Corylifol-A.html HYPERLINK https:/www.MedChemE/Cryptotanshinone.html Cryptotanshinone(Corylifol-A; Corylinin) Cat. No.: HY-N0897 (Cryptotanshinon; Tanshinone c) Cat. No.: HY-N0174Corylifol A inhibits IL-6-induced STAT3activation and phosphorylation, with an IC of500.81 M.Cryptotanshinone is a

56、 natural compound extractedfrom the root of Salvia miltiorrhiza Bunge thatshows antitumor activities. Cryptotanshinoneinhibits STAT3 with an IC of 4.6 M.50Purity: 99.75%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98.46%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg,

57、 50 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/Cucurbitacin-I.html Cucurbitacin HYPERLINK https:/www.MedChemE/Cucurbitacin-I.html HYPERLINK https:/www.MedChemE/Cucurbitacin-I.html I(Elatericin B; JSI-124; NSC-521777) Cat. No.: HY-N1405 HYPERLINK https:/www.MedChemE/curculigoside.html Curculigosi

58、deCat. No.: HY-N0705Cucurbitacin I is a natural selective inhibitor ofJAK2/STAT3, with potent anti-cancer activity.Curculigoside is the main saponin in C. orchioide,exerts significant antioxidant, anti-osteoporosis,antidepressant and neuroprotection effects.Curculigoside possesses significant anti-a

59、rthriticeffects in vivo and in vitro via regulation of theJAK/STAT/NF-B signaling pathway.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/danvat

60、irsen.html Danvatirsen(AZD 9150) Cat. No.: HY-145729 HYPERLINK https:/www.MedChemE/debio-0617b.html Debio HYPERLINK https:/www.MedChemE/debio-0617b.html HYPERLINK https:/www.MedChemE/debio-0617b.html 0617BCat. No.: HY-108417Danvatirsen is an antisense oligonucleotidetargeting STAT3 with potential an