JNK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/JNK.html JNKc-Jun N-terminal kinaseJNK (c-Jun N-terminal kinase), a kinase subfamily belonging to the MAPK, is activated in response to various stress stimuli andpossesses a wide variety of regulatory functions. The JNK family of serine/threonine protein kinase

2、s comprises three isoforms (JNK1,JNK2 and JNK3). JNKs are involved in the emergence and progression of diverse pathologies such as neurodegenerative,cardiovascular and metabolic disorders as well as inflammation and cancer.Similar to the other MAP kinases, JNKs are activated by a phosphorylation cas

3、cade generally involving two types of upstreamkinases, the so-called MAP kinase kinase kinases (MAP3K, MKKK) and the MAP kinase kinases (MAP2K; MKK). At the MAP2K level,JNKs are activated by MKK4 and MKK7, the former is a common activator of the JNK and the p38 MAP kinase signaling pathway.The JNK c

4、ascade shares various intersection points with other pathways making it a part of a complex signaling network.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/JNK.html JNK HYPERLINK https:/www.MedChemE/Targets/JNK.html HYPERLINK https:/www.MedChemE/Targets/JNK.html Inhibitors HYPERLINK https:/ww

5、w.MedChemE/Targets/JNK.html HYPERLINK https:/www.MedChemE/Targets/JNK.html & HYPERLINK https:/www.MedChemE/Targets/JNK.html HYPERLINK https:/www.MedChemE/Targets/JNK.html Activators HYPERLINK https:/www.MedChemE/minus-zuonin-a.html (-)-Zuonin HYPERLINK https:/www.MedChemE/minus-zuonin-a.html HYPERLI

6、NK https:/www.MedChemE/minus-zuonin-a.html A(D-Epigalbacin) Cat. No.: HY-N7394A HYPERLINK https:/www.MedChemE/e-osmundacetone.html (E)-OsmundacetoneCat. No.: HY-N1966(-)-Zuonin A (D-Epigalbacin), a naturallyoccurring lignin, is a potent, selective JNKsinhibitor, with IC s of 1.7 M, 2.9 M and 1.7450M

7、 for JNK1, JNK2 and JNK3, respectively.(E)-Osmundacetone is the isomer of Osmundacetone.Osmundacetone significantly suppresses thephosphorylation of MAPKs, including JNK, ERK, andp38 kinases. Osmundacetone has a neuroprotectiveeffect against oxidative stress.Purity: 99.84%Clinical Data: No Developme

8、nt ReportedSize: 1 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/actein.html Actein HYPERLINK https:/www.MedChemE/actein.html HYPERLINK https:/www.MedChemE/aeg3482.html AEG3482Cat. No.: HY-N6872 Cat. No.: HY-107599Actein is a trite

9、rpene glycoside isolated from therhizomes of Cimicifuga foetida. Acteinsuppresses cell proliferation, induces autophagyand apoptosis through promoting ROS/JNKactivation, and blunting AKT pathway in humanbladder cancer. Actein has little toxicity in vivo.AEG3482 is a potent antiapoptotic compound tha

10、tinhibits Jun kinase (JNK) activity throughinduced expression of heat shock protein 70(HSP70). AEG3482 directly binds HSP90, therebyfacilitating HSF1-dependent expression of HSP70and HSP25.Purity: 98.58%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.21%Clinical Data: No Development Repor

11、tedSize: 5 mg HYPERLINK https:/www.MedChemE/aloisine-a.html Aloisine HYPERLINK https:/www.MedChemE/aloisine-a.html HYPERLINK https:/www.MedChemE/aloisine-a.html A(RP107) Cat. No.: HY-112363 HYPERLINK https:/www.MedChemE/Anisomycin.html Anisomycin(Flagecidin; Wuningmeisu C) Cat. No.: HY-18982Aloisine

12、 A (RP107) is a a potent cyclin-dependentkinase (CDK) inhibitor with IC s of 0.15 M, 0.1250M, 0.4 M, 0.16 M for CDK1/cyclin B, CDK2/cyclinA, CDK2/cyclin E, CDK5/p35, respectively. AloisineA ininhibits GSK-3 (IC =0.5 M) and GSK-350(IC =1.5 M).50Purity: 98%Clinical Data: No Development ReportedSize: 1

13、 mg, 5 mgAnisomycin is a potent protein synthesis inhibitorwhich interferes with protein and DNA synthesis byinhibiting peptidyl transferase or the 80Sribosome system. Anisomycin is a JNK activator,which increases phospho-JNK. Anisomycin is abacterial antibiotic.Purity: 98.59%Clinical Data: No Devel

14、opment ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AS601245.html AS601245 HYPERLINK https:/www.MedChemE/AS601245.html HYPERLINK https:/www.MedChemE/Astragaloside-IV.html Astragaloside HYPERLINK https:/www.MedChemE/Astragaloside-IV.html HYPERLINK https:/www.MedChemE/A

15、stragaloside-IV.html IVCat. No.: HY-11010 Cat. No.: HY-N0431AS601245 is an orally active, selective, ATPcompetitive JNK (c-Jun NH2-terminal proteinkinase) inhibitor with IC s of 150, 220, and 70 nM50for three JNK human isoforms (hJNK1, hJNK2, andhJNK3), respectively.Astragaloside IV, an active compo

16、nent isolatedfrom Astragalus membranaceus, suppresses theactivation of ERK1/2 and JNK, and downregulatesmatrix metalloproteases (MMP)-2, (MMP)-9 inMDA-MB-231 breast cancer cells.Purity: 98.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data

17、: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AS-602801.html Bentamapimod HYPERLINK https:/www.MedChemE/AS-602801.html HYPERLINK https:/www.MedChemE/BI-78D3.html BI-78D3(AS 602801) Cat. No.: HY-14761Cat. No.: HY-10366Bentamapimod (AS 602801) is an ATP-

18、competitiveJNK inhibitor with IC of 80 nM, 90 nM, and 23050nM for JNK1, JNK2, and JNK3, respectively.BI-78D3 functions as a substrate competitiveinhibitor of JNK, inhibit the JNK kinase activity(IC =280 nM).50Purity: 99.52%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1

19、 gPurity: 99.49%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/cc-401.html CC-401Cat. No.: HY-13022A HYPERLINK https:/www.MedChemE/CC-401-hydrochloride.html CC-401 HYPER

20、LINK https:/www.MedChemE/CC-401-hydrochloride.html HYPERLINK https:/www.MedChemE/CC-401-hydrochloride.html hydrochloride(CC401 HCl) Cat. No.: HY-13022CC-401 is a potent inhibitor of all three forms ofJNK with K of 25 to 50 nM.iCC-401 hydrochloride is a potent inhibitor of allthree forms of JNK with

21、K of 25 to 50 nM.iPurity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mgPurity: 99.46%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/cc-90001.html CC-90001Cat. No.: HY-138304 HYPERLINK https:/www.MedChemE/D-JNKI-1.html D-JNKI-1(AM-111; XG-102) Cat. No.: HY-P0069C

22、C-90001 is a potent, selective and orally activeinhibitor of c-Jun N-terminal kinase (JNK).CC-90001 shows 12.9-fold selectivity for JNK1over JNK2 in a cell-based model. CC-90001 can beused for the research of idiopathic pulmonaryfibrosis.D-JNKI-1 (AM-111) is a highly potent andcell-permeable peptide

23、 inhibitor of JNK.Purity: 99.85%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.07%Clinical Data: Phase 3Size: 1 mg, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/DB07268.html DB07268 HYPERLINK https:/www.MedChemE/DB07268.html HYPERLINK https:/www.MedChemE/dtp3-tfa.html DT

24、P3 HYPERLINK https:/www.MedChemE/dtp3-tfa.html HYPERLINK https:/www.MedChemE/dtp3-tfa.html TFACat. No.: HY-15737 Cat. No.: HY-100538ADB07268 is a potent and selective JNK1 inhibitorwith an IC value of 9 nM.50DTP3 TFA is a potent and selective GADD45/MKK7(growth arrest and DNA-damage-inducible/mitoge

25、n-activated protein kinase kinase 7)inhibitor. DTP3 TFA targets an essential,cancer-selective cell-survival module downstreamof the NF-B pathway.Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.75%Clinical Data: No Development ReportedSize: 1

26、0 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/esculentoside-h.html Esculentoside HYPERLINK https:/www.MedChemE/esculentoside-h.html HYPERLINK https:/www.MedChemE/esculentoside-h.html H HYPERLINK https:/www.MedChemE/esculentoside-h.html HYPERLINK https:/www.MedChemE/Ginse

27、noside-Re.html Ginsenoside HYPERLINK https:/www.MedChemE/Ginsenoside-Re.html HYPERLINK https:/www.MedChemE/Ginsenoside-Re.html ReCat. No.: HY-N2205(Ginsenoside B2; Panaxoside Re; Sanchinoside Re) Cat. No.: HY-N0044Esculentoside H (EsH) is a saponin isolated fromthe root extract of perennial plant Ph

28、ytolaccaesculenta. Esculentoside H (EH) has anti-tumoractivity, the mechanism is related to the capacityfor TNFrelease.Ginsenoside Re (Ginsenoside B2) is an extract fromPanax notoginseng. Ginsenoside Re decreases the-amyloid protein (A). Ginsenoside Re plays arole in antiinflammation through inhibit

29、ion ofJNK and NF-B.Purity: 98.02%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98.15%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/guggulsterone.html Guggulsterone HYPERLINK https:/www.MedChemE/guggulsterone.html HYPERLINK https:/www.MedChemE/indi

30、rubin-3-oxime.html Indirubin-3-oxime(Z/E-Guggulsterone) Cat. No.: HY-107738 (IDR3O; I3O) Cat. No.: HY-139254Guggulsterone is a plant sterol derived from thegum resin of the tree Commiphora wightii.Indirubin-3-oxime (IDR3O), a synthetic derivativeof indirubin, is a potent inhibitor ofcyclin-dependent

31、 kinases (CDKs) and glycogensynthase kinase 3 (GSK3).Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.49%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/IQ-1S-fre

32、e-acid.html IQ-1S HYPERLINK https:/www.MedChemE/IQ-1S-free-acid.html HYPERLINK https:/www.MedChemE/IQ-1S-free-acid.html free HYPERLINK https:/www.MedChemE/IQ-1S-free-acid.html HYPERLINK https:/www.MedChemE/IQ-1S-free-acid.html acid HYPERLINK https:/www.MedChemE/IQ-1S-free-acid.html HYPERLINK https:/

33、www.MedChemE/iq-3.html IQ-3Cat. No.: HY-100233 Cat. No.: HY-107600IQ-1S free acid is a prospective inhibitor ofNF-B/activating protein 1 (AP-1) activity with anIC of 2.30.41 M. IQ-1S free acid has binding50affinity (K values) in the nanomolar range fordall three JNKs with K s of 100 nM, 240 nM, andd

34、360 nM for JNK3, JNK1, and JNK2, respectively.IQ-3 is a specific inhibitor of the c-JunN-terminal kinase (JNK) family, with preferencefor JNK3. IQ-3 exhibits K values of 0.24 M,d0.29 M and 0.066 M for JNK1, JNK2 and JNK3,respectively.Purity: 99.35%Clinical Data: No Development ReportedSize: 5 mg, 10

35、 mg, 25 mg, 50 mg, 100 mgPurity: 98.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Isovitexin.html Isovitexin(Saponaretin; Homovitexin) Cat. No.: HY-N0773 HYPERLINK https:/www.MedChemE/j30-8.html J30-8Cat. No.: HY-125838Isov

36、itexin is a flavonoid isolated from rice hullsof Oryza sativa, possesses anti-inflammatory andanti-oxidant activities; Isovitexin acts like aJNK1/2 inhibitor and inhibits the activation ofNF-B.J30-8 is a potent and isoform-selective inhibitorof c-Jun N-terminal kinase 3 (JNK3) with an IC50of 40 nM,

37、which 2500-fold isoform selectivityagainst JNK11 and JNK22. J30-8 exhibitsneuroprotective activity in vitro and potentialfor the treatment of neurodegenerative diseases.Purity: 99.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development Re

38、portedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/jip-1-153-163.html JIP-1(153-163)(T1-JIP) Cat. No.: HY-P1191 HYPERLINK https:/www.MedChemE/jip-1-153-163-tfa.html JIP-1(153-163) HYPERLINK https:/www.MedChemE/jip-1-153-163-tfa.html HYPERLINK https:/www.MedChemE/jip-1-153-163-tfa.html TFA(T1-JIP T

39、FA) Cat. No.: HY-P1191AJIP-1(153-163) (TI-JIP) is a peptide inhibitor ofc-JNK, based on residues 153-163 ofJNK-interacting protein-1 (JIP-1) (Modifications:Phe-11 = C-terminal amide).JIP-1(153-163) TFA (TI-JIP TFA) is a peptideinhibitor of c-JNK, based on residues 153-163 ofJNK-interacting protein-1

40、 (JIP-1) (Modifications:Phe-11 = C-terminal amide).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/jnk-inhibitor-viii.html JNK HYPERLINK https:/www.MedChemE/jnk-inhibitor-viii.html HYPERL

41、INK https:/www.MedChemE/jnk-inhibitor-viii.html Inhibitor HYPERLINK https:/www.MedChemE/jnk-inhibitor-viii.html HYPERLINK https:/www.MedChemE/jnk-inhibitor-viii.html VIII HYPERLINK https:/www.MedChemE/jnk-inhibitor-viii.html HYPERLINK https:/www.MedChemE/jnk-in-7.html JNK-IN-7(TCS JNK 6o) Cat. No.:

42、HY-107598 (JNK inhibitor) Cat. No.: HY-15617JNK Inhibitor VIII (TCS JNK 6o) is a c-JunN-terminal kinases (JNK-1, -2, and -3) inhibitorwith K values of 2 nM, 4 nM, 52 nM, respectively,iand has IC values of 45 nM and 160 nM for JNK-150and -2, respectively.JNK-IN-7 is a potent JNK inhibitor with IC of5

43、01.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3,respectively.Purity: 99.56%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mgPurity: 98.41%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/JNK-IN-8.html JNK-IN-8 HYPERLINK http

44、s:/www.MedChemE/JNK-IN-8.html HYPERLINK https:/www.MedChemE/jnk3-inhibitor-1.html JNK3 HYPERLINK https:/www.MedChemE/jnk3-inhibitor-1.html HYPERLINK https:/www.MedChemE/jnk3-inhibitor-1.html inhibitor-1(JNK Inhibitor XVI) Cat. No.: HY-13319Cat. No.: HY-139624JNK-IN-8 (JNK Inhibitor XVI) is a potent

45、JNKinhibitor with IC s of 4.7 nM, 18.7 nM, and 1 nM50for JNK1, JNK2, and JNK3, respectively.JNK3 inhibitor-1 is a potent and selective JNK3inhibitor (IC = 0.005 M). JNK3 inhibitor-1 is50orally bioavailable and brain penetrant.Purity: 99.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg

46、, 5 mg, 10 mg, 50 mg, 100 mg, 200 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/jtp10-r9-tfa.html JTP10-R9 HYPERLINK https:/www.MedChemE/jtp10-r9-tfa.html HYPERLINK https:/www.MedChemE/jtp10

47、-r9-tfa.html TFA HYPERLINK https:/www.MedChemE/jtp10-r9-tfa.html HYPERLINK https:/www.MedChemE/jtp10-tati-tfa.html JTP10-TATi HYPERLINK https:/www.MedChemE/jtp10-tati-tfa.html HYPERLINK https:/www.MedChemE/jtp10-tati-tfa.html TFACat. No.: HY-P2247 Cat. No.: HY-P2246JTP10-R9 TFA is a selective JNK2 p

48、eptideinhibitor, with an IC of 89 nM, exhibiting5010-fold selectivity for JNK2 over JNK1 and JNK3.JTP10-TATi TFA is a selective JNK2 peptideinhibitor, with an IC of 92 nM, exhibiting5010-fold selectivity for JNK2 over JNK1 and JNK3.Purity: 99.80%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

49、, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Juglanin.html Juglanin HYPERLINK https:/www.MedChemE/Juglanin.html HYPERLINK https:/www.MedChemE/L-JNKI-1.html L-JNKI-1Cat. No.: HY-N3442 Cat. No.: HY-P0069AJuglanin, a natural occu

50、rring flavonoid, is a JNKacticator, with inflammation and anti-tumoractivities. Juglanin can induce apoptosis andautophagy on human breast cancer cells.L-JNKI-1 is a cell-permeable peptide inhibitorspecific for JNK.Purity: 99.90%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 96.05%Cli

51、nical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Loureirin_B.html Loureirin HYPERLINK https:/www.MedChemE/Loureirin_B.html HYPERLINK https:/www.MedChemE/Loureirin_B.html B HYPERLINK https:/www.MedChemE/Loureirin_B.html HYPERLINK https:/www.MedChemE/mpt0

52、b392.html MPT0B392Cat. No.: HY-N1504 Cat. No.: HY-101287Loureirin B, a flavonoid extracted from Dracaenacochinchinensis, is an inhibitor of plasminogenactivator inhibitor-1 (PAI-1), with an IC of5026.10M; Loureirin B also inhibits K , theATPphosphorylation of ERK and JNK, and hasanti-diabetic activi

53、ty.MPT0B392, an orally active quinoline derivative,induces c-Jun N-terminal kinase (JNK) activation,leading to apoptosis.Purity: 99.16%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:

54、/www.MedChemE/ova-e1-peptide.html OVA-E1 HYPERLINK https:/www.MedChemE/ova-e1-peptide.html HYPERLINK https:/www.MedChemE/ova-e1-peptide.html peptide HYPERLINK https:/www.MedChemE/ova-e1-peptide.html HYPERLINK https:/www.MedChemE/ova-e1-peptide-tfa.html OVA-E1 HYPERLINK https:/www.MedChemE/ova-e1-pep

55、tide-tfa.html HYPERLINK https:/www.MedChemE/ova-e1-peptide-tfa.html peptide HYPERLINK https:/www.MedChemE/ova-e1-peptide-tfa.html HYPERLINK https:/www.MedChemE/ova-e1-peptide-tfa.html TFACat. No.: HY-P2319 Cat. No.: HY-P2319AOVA-E1 peptide, is an antagonist variant ofSIINFEKL OVA (257-264). OVA-E1 p

56、eptide, activatesthe p38 and JNK cascades similarly in mutant andwild-type thymocytes.OVA-E1 peptide TFA, is an antagonist variant ofSIINFEKL OVA (257-264). OVA-E1 peptide, activatesthe p38 and JNK cascades similarly in mutant andwild-type thymocytes.Purity: 98%Clinical Data: No Development Reported

57、Size: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/polyphyllin-i.html Polyphyllin HYPERLINK https:/www.MedChemE/polyphyllin-i.html HYPERLINK https:/www.MedChemE/polyphyllin-i.html I HYPERLINK https:/www.MedChemE/polyphyllin-i.html HYPERLIN

58、K https:/www.MedChemE/salicortin.html SalicortinCat. No.: HY-N0047 Cat. No.: HY-123503Polyphyllin I is a bioactive constituent extractedfrom Paris polyphylla, has strong anti-tumoractivity. Polyphyllin I is an activator of theJNK signaling pathway and is an inhibitor ofPDK1/Akt/mTOR signaling. Polyp

59、hyllin I inducesautophagy, G2/M phase arrest and apoptosis.Salicortin, a phenolic glycoside, has beenisolated from many plants such as Populus and Salixspecies. Salicortin inhibits osteoclastdifferentiation and bone resorption bydown-regulating JNK and NF-B/NFATc1 signalingpathways.Purity: 99.61%Cli

60、nical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 98%Clinical Data:Size: 100 g, 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/sesamolin.html Sesamolin HYPERLINK https:/www.MedChemE/sesamolin.html HYPERLINK https:/www.MedChemE/SP600125.html SP600125Cat. No.: HY-N0809 Cat. No