1、 HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html p38 HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html MAPKThe p38 MAPK family consists of highly conserved proline-directed serine-threonine protein kinases that are activated in responseto a n

2、umber many growth factors, cytokines, and chemotactic substances, such as vascular endothelial growth factor (VEGF),fibroblast growth factor (FGF), PDGF, TNF, interleukins, lipopolysaccharide (LPS) and formyl-methionyl-leucyl-phenylalanine (fMLP).It is well known that p38 is involved in inflammation

3、, apoptosis, cardiomyocyte hypertrophy and cell differentiation.The p38 MAPK family is composed of four proteins: p38 (encoded by the gene Mapk14), p38 (Mapk11), p38 (Mapk12), andp38 (Mapk13). Their coding genes have a distinct tissue distribution and they appear differentially expressed, being Mapk

4、14 themost highly expressed. p38 MAPKs are substrates for three MAP2K (MKK6, MKK3, and MKK4). The contribution of each of theseMAP2K to p38 MAPKs activation depends on the stimulus and the cell type. The MAP3Ks that lead to p38 MAPKs activation areASK1, DLK1, TAK1, TAO1, TAO2, TPL2, MLK3, MEKK3, MEK

5、K4, and ZAK1.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html p38 HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html MAPK HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html Inh

6、ibitors, HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html Activators HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html & HYPERLINK https:/www.MedChemE/Targets/p38 MAPK.html HYPERLINK https:/w

7、ww.MedChemE/Targets/p38 MAPK.html Modulators HYPERLINK https:/www.MedChemE/e-osmundacetone.html (E)-Osmundacetone HYPERLINK https:/www.MedChemE/e-osmundacetone.html HYPERLINK https:/www.MedChemE/rac-hesperetin.html (Rac)-HesperetinCat. No.: HY-N1966 Cat. No.: HY-N0168A(E)-Osmundacetone is the isomer

8、 of Osmundacetone.Osmundacetone significantly suppresses thephosphorylation of MAPKs, including JNK, ERK, andp38 kinases. Osmundacetone has a neuroprotectiveeffect against oxidative stress.(Rac)-Hesperetin is the racemate of Hesperetin.Hesperetin is a natural flavanone, and acts as apotent and broad

9、-spectrum inhibitor against humanUGT activity. Hesperetin induces apoptosis viap38 MAPK activation.Purity: 99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.20%Clinical Data: No Development ReportedSize: 100 mg HYPERLINK https:/www.MedChemE/rac-hesperetin-13c-d3.ht

10、ml (Rac)-Hesperetin-13C,d3 HYPERLINK https:/www.MedChemE/rac-hesperetin-13c-d3.html HYPERLINK https:/www.MedChemE/rac-hesperetin-d3.html (Rac)-Hesperetin-d3Cat. No.: HY-N0168AS1 Cat. No.: HY-N0168AS(Rac)-Hesperetin-13C,d3 is the 13C- and deuteriumlabeled. (Rac)-Hesperetin is the racemate ofHespereti

11、n. Hesperetin is a natural flavanone, andacts as a potent and broad-spectrum inhibitoragainst human UGT activity. Hesperetin inducesapoptosis via p38 MAPK activation.(Rac)-Hesperetin-d3 is the deuterium labeled(Rac)-Hesperetin. (Rac)-Hesperetin is the racemateof Hesperetin. Hesperetin is a natural f

12、lavanone,and acts as a potent and broad-spectrum inhibitoragainst human UGT activity. Hesperetin inducesapoptosis via p38 MAPK activation.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/

13、4-hydroxylonchocarpin.html 4-HydroxylonchocarpinCat. No.: HY-N2208 HYPERLINK https:/www.MedChemE/5-6-7-trimethoxyflavone.html 5,6,7-Trimethoxyflavone(Baicalein trimethyl ether) Cat. No.: HY-1103984-Hydroxylonchocarpin is a chalcone compound froman extract of Psoralea corylifolia.4-Hydroxylonchocarpi

14、n increases phosphorylation ofp38 MAPK, JNK and ERK.5,6,7-Trimethoxyflavone is a novel p38- MAPKinhibitor with an anti-inflammatory effect.5,6,7-Trimethoxyflavone is isolated from severalplants including Zeyhera tuberculosa, Callicarpajaponica, and Kickxia lanigera.Purity: 92.14%Clinical Data: No De

15、velopment ReportedSize: 5 mg, 10 mgPurity: 98.76%Clinical Data:Size: 10 mg HYPERLINK https:/www.MedChemE/Acumapimod.html Acumapimod HYPERLINK https:/www.MedChemE/Acumapimod.html HYPERLINK https:/www.MedChemE/SB-203580.html Adezmapimod(BCT197) Cat. No.: HY-16715 (SB 203580; RWJ 64809) Cat. No.: HY-10

16、256Acumapimod (BCT197) is an orally active p38MAP kinase inhibitor, with an IC of less than501 M for p38.Adezmapimod (SB 203580) is a selective andATP-competitive p38 MAPK inhibitor with IC s50of 50 nM and 500 nM for SAPK2a/p38 andSAPK2b/p382, respectively. Adezmapimod inhibitsLCK, GSK3 and PKB with

17、 IC s of 100-500-fold50higher than that for SAPK2a/p38.Purity: 99.63%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/SB-203580-hydrochloride.html

18、Adezmapimod HYPERLINK https:/www.MedChemE/SB-203580-hydrochloride.html HYPERLINK https:/www.MedChemE/SB-203580-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/SB-203580-hydrochloride.html HYPERLINK https:/www.MedChemE/al-8697.html AL HYPERLINK https:/www.MedChemE/al-8697.html HYPERLIN

19、K https:/www.MedChemE/al-8697.html 8697(SB 203580 hydrochloride; RWJ 64809 hydrochloride) Cat. No.: HY-10256ACat. No.: HY-108645Adezmapimod (SB 203580) hydrochloride is aselective and ATP-competitive p38 MAPKinhibitor with IC s of 50 nM and 500 nM for50SAPK2a/p38 and SAPK2b/p382, respectively.AL 869

20、7 is a specific and orally active p38MAPK inhibitor with an IC of 6 nM. AL 869750displays 14-fold greater inhibition of p38compared to p38 (IC =82 nM), and 300-fold50selectivity for p38 over a panel of 91 kinases.Anti-inflammatory activity.Purity: 99.71%Clinical Data: No Development ReportedSize: 10

21、 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.49%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/AMG-47a.html AMG-47a HYPERLINK https:/www.MedChemE/AMG-47a.html HYPERLINK https:/www.MedChemE/amg-5

22、48.html AMG-548Cat. No.: HY-18303 Cat. No.: HY-108642AMG-47a is a potent and orally activelymphocyte-specific protein tyrosine kinase(Lck) inhibitor, with an IC of 0.2 nM. AMG-47a50also inhibits VEGF2, p38, Jak3 and MLR andIL-2 with IC s of 1 nM, 3 nM, 72 nM, 30 nM and 2150nM, respectively.Purity: 9

23、8.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgAMG-548, an orally active and selective p38inhibitor (K=0.5 nM), shows slightly selectiveiover p38 (K=36 nM) and 1000 fold selectiveiagainst p38 and p38. AMG 548 is also extremelypotent in the inhibition of whole b

24、lood LPSstimulated TNF (IC =3 nM).50Purity: 99.0%Clinical Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/amg-548-dihydrochloride.html AMG-548 HYPERLINK https:/www.MedChemE/amg-548-dihydrochloride.html HYPERLINK https:/www.MedChemE/amg-548-dihydrochloride.html dihydrochloride HYPERLINK https:/ww

25、w.MedChemE/amg-548-dihydrochloride.html HYPERLINK https:/www.MedChemE/amg-548-hydrochloride.html AMG-548 HYPERLINK https:/www.MedChemE/amg-548-hydrochloride.html HYPERLINK https:/www.MedChemE/amg-548-hydrochloride.html hydrochlorideCat. No.: HY-108642B Cat. No.: HY-108642AAMG-548 dihydrochloride, an

26、 orally active andselective p38 inhibitor (K=0.5 nM), showsislightly selective over p38 (K=36 nM) andi1000 fold selective against p38 and p38.AMG-548 hydrochloride, an orally active andselective p38 inhibitor (K=0.5 nM), showsislightly selective over p38 (K=36 nM) andi1000 fold selective against p38

27、 and p38.Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/andrograpanin.html Andrograpanin HYPERLINK https:/www.MedChemE/andrograpanin.html HYPE

28、RLINK https:/www.MedChemE/anti-inflammatory-agent-7.html Anti-inflammatory HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-7.html HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-7.html agent HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-7.html HYPERLINK https:/www.MedChemE/anti-i

29、nflammatory-agent-7.html 7Cat. No.: HY-N9388 Cat. No.: HY-139844Andrograpanin, a bioactive compound fromAndrographis paniculata, exhibitsanti-inflammatory and anti-infectiousproperties.Anti-inflammatory agent 7 inhibits proinflammatorycytokines by blocking the NF-B/MAPK signalingpathway in LPS-treat

30、ed RAW 264.7 cells as well asmice.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ask1-in-1-1.html ASK1-IN-1 HYPERLINK https:/www.MedChemE/ask1-in-1-1.html HYPERLINK https:/www.Me

31、dChemE/AZD7624.html AZD7624Cat. No.: HY-133554 Cat. No.: HY-103672ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosissignal-regulating kinase 1) inhibitor, with goodpotency (cell IC =138 nM; Biochemical =2150 IC50nM).AZD7624 is an inhaled p38 inhibitor, with potentanti-inflammatory activity.Purity: 99.79%C

32、linical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.08%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/Bakuchiol.html Bakuchiol HYPERLINK https:/www.MedChemE/Bakuchiol.html HYPERLINK https:/www.MedChemE/sos1-in

33、-2.html BI-3406(S)-(+)-Bakuchiol) Cat. No.: HY-N0235Cat. No.: HY-125817Bakuchiol is a phytoestrogen isolated from theseeds of Psoralea corylifolia L; has anti-tumoreffects.BI-3406 (compound I-6) is an orally active, highlypotent and selective inhibitor of the interactionbetween KRAS and Son of Seven

34、less 1 (SOS1) withan IC of 6 nM. BI-3406 potently reduces the50formation of GTP-loaded KRAS, and inhibits MAPKpathway signaling.Purity: 99.25%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25

35、 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/bisabolangelone.html Bisabolangelone HYPERLINK https:/www.MedChemE/bisabolangelone.html HYPERLINK https:/www.MedChemE/BMS-582949-hydrochloride.html BMS-582949 HYPERLINK https:/www.MedChemE/BMS-582949-hydrochloride.html HYPERLINK https:/w

36、ww.MedChemE/BMS-582949-hydrochloride.html hydrochlorideCat. No.: HY-N4233 Cat. No.: HY-14305ABisabolangelone, a sesquiterpene derivative, isisolated from the roots of Osterici Radix.BMS-582949 hydrochloride is an orally active andhighly selective p38 MAPK inhibitor, with anIC of 13 nM. BMS-582949 hy

37、drochloride displays a50significantly improved pharmacokinetic profile andis effective in inflammatory disease.Purity: 98.22%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98.29%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/c1

38、6-paf.html C16-PAF(PAF (C16) Cat. No.: HY-108635 HYPERLINK https:/www.MedChemE/chicanine.html ChicanineCat. No.: HY-N2270C16-PAF (PAF (C16), a phospholipid mediator, is aplatelet-activating factor and ligand for PAFG-protein-coupled receptor (PAFR). C16-PAFexhibits anti-apoptotic effect and inhibits

39、caspase-dependent death by activating the PAFR.Chicanine is a lignan compound of Schisandrachinesis, inhibits LPS-induced phosphorylation ofp38 MAPK, ERK 1/2 and IB-, withanti-inflammatory activity.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98%Clinical Da

40、ta: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cornuside.html Cornuside HYPERLINK https:/www.MedChemE/cornuside.html HYPERLINK https:/www.MedChemE/cycloartenol.html CycloartenolCat. No.: HY-N0631 Cat. No.: HY-N7255Cornuside is a secoiridoid glucoside isolated fromthe frui

41、t of Cornus officinalis Sieb. et Zucc.,which is a traditional oriental medicine fortreating inflammatory diseases and invigoratingblood circulation.Cycloartenol, a phytosterol compound, is one ofthe key precusor substances for biosynthesis ofnumerous sterol compounds. Cycloartenol inhibitsthe migrat

42、ion of glioma cells and suppresses thephosphorylation of the p38 MAP kinase.Purity: 99.26%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Dehydrocorydaline.html Dehydrocorydaline HYPERLINK https:

43、/www.MedChemE/Dehydrocorydaline.html HYPERLINK https:/www.MedChemE/Dehydrocorydaline-chloride.html Dehydrocorydaline HYPERLINK https:/www.MedChemE/Dehydrocorydaline-chloride.html HYPERLINK https:/www.MedChemE/Dehydrocorydaline-chloride.html chloride(13-Methylpalmatine) Cat. No.: HY-N0674 (13-Methylp

44、almatine chloride) Cat. No.: HY-N0674ADehydrocorydaline (13-Methylpalmatine) is analkaloid that regulates protein expression ofBax, Bcl-2; activates caspase-7, caspase-8, andinactivates PARP. Dehydrocorydaline elevates p38MAPK activation. Anti-inflammatory andanti-cancer activities.Dehydrocorydaline

45、 chloride (13-Methylpalmatinechloride) is an alkaloid that regulates proteinexpression of Bax, Bcl-2; activates caspase-7,caspase-8, and inactivates PARP.Dehydrocorydaline chloride elevates p38 MAPKactivation.Purity: 99.01%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99

46、.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/dehydrocorydaline-nitrate.html Dehydrocorydaline HYPERLINK https:/www.MedChemE/dehydrocorydaline-nitrate.html HYPERLINK https:/www.MedChemE/dehydrocorydaline-nitrate.html nitrate HYPERLINK https:/ww

47、w.MedChemE/dehydrocorydaline-nitrate.html HYPERLINK https:/www.MedChemE/dihydrocaffeic-acid.html Dihydrocaffeic HYPERLINK https:/www.MedChemE/dihydrocaffeic-acid.html HYPERLINK https:/www.MedChemE/dihydrocaffeic-acid.html acid(13-Methylpalmatine nitrate) Cat. No.: HY-N4238 (3,4-Dihydroxy-benzeneprop

48、anoic acid) Cat. No.: HY-N2406Dehydrocorydaline nitrate (13-Methylpalmatinenitrate) is an alkaloid. Dehydrocorydalineregulates protein expression of Bax, Bcl-2;activates caspase-7, caspase-8, and inactivatesPARP. Dehydrocorydaline nitrate elevates p38MAPK activation.Dihydrocaffeic acid is a phenolic

49、 acid found inGynura bicolor, reduces phosphorylation of MAPKp38 and prevent UVB-induced skin damage.Antioxidant potential and anti-inflammatoryactivity.Purity: 99.89%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg4 Te

50、l: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/SB-681323.html Dilmapimod(SB-681323; GW 681323) Cat. No.: HY-10404 HYPERLINK https:/www.MedChemE/Doramapimod.html Doramapimod(BIRB 796) Cat. No.: HY-10320Dilmapimod (SB-681323) is a potent p38 MAPKinhibitor that pot

51、entially suppresses inflammationin chronic obstructive pulmonary disease.Purity: 99.56%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgDoramapimod (BIRB 796) is an orally active, highlypotent p38 MAPK inhibitor, which has an IC50for p38=38 nM, for p38=65 nM, for p38=200 nM,and for p38=5

52、20 nM. Doramapimod has picomolaraffinity for p38 kinase (K =0.1 nM). Doramapimoddalso inhibits B-Raf with an IC of 83 nM.50Purity: 99.88%Clinical Data: Phase 2Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/emprumapimod.html Emprumapimod(PF-07265803) Cat. No.: HY-145564

53、HYPERLINK https:/www.MedChemE/eo-1428.html EO HYPERLINK https:/www.MedChemE/eo-1428.html HYPERLINK https:/www.MedChemE/eo-1428.html 1428Cat. No.: HY-108647Emprumapimod is a potent, orally bioavailable andselective inhibitor of p38 MAPK directlyinhibits LPS-induced IL-6 production fromRPMI-8226 cell

54、(IC =100 pM). Emprumapimod can be50used for the research of dilated cardiomyopathyand acute inflammatory pain.EO 1428 is a highly specific inhibitor of p38 ofthe aminobenzophenone class. EO 1428 (1 M )markedly attenuates LPS-induced tumor necrosisfactor -converting enzyme (TACE) activityup-regulatio

55、n.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/esculin.html Esculin HYPERLINK https:/www.MedChemE/esculin.html HYPERLINK https:/www.MedChemE/ew-7195.html EW-7195Cat. No.: HY-N0188 Cat.

56、 No.: HY-18766Esculin, a fluorescent coumarin glucoside, is anactive ingredient of ash bark. Esculin amelioratescognitive impairment in experimental diabeticnephropathy (DN), and exerts antioxidative stressand antiinflammatory effects, via the MAPKsignaling pathway.EW-7195 is a potent and selective

57、ALK5 (TGFR1)inhibitor with an IC of 4.83 nM. EW-7195 has50300-fold selectivity for ALK5 over p38.EW-7195 efficiently inhibits TGF-1-induced Smadsignaling, epithelial-to-mesenchymal transition(EMT) and breast tumour metastasis to the lung.Purity: 99.19%Clinical Data: No Development ReportedSize: 10 m

58、M 1 mL, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html Ferulic HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html acid HYPERLINK https:/www.Med

59、ChemE/Ferulic_acid_methyl_ester.html HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html methyl HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html ester HYPERLINK https:/www.MedChemE/Ferulic_acid_methyl_ester.html HYPERL

60、INK https:/www.MedChemE/FR_167653.html FR HYPERLINK https:/www.MedChemE/FR_167653.html HYPERLINK https:/www.MedChemE/FR_167653.html 167653(Methyl ferulate) Cat. No.: HY-W018643 (FR 167653 sulfate) Cat. No.: HY-18754AFerulic acid methyl ester (Methyl ferulate) is aderivative of ferulic acid, isolated