MAP3K-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/MAP3K.html MAP3KMAP kinase kinase kinase, MEKK, MAPKKKMAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, provide specificity forstimulus-dependent activation of MAP2K-MAPK pathways through unique protein-protein inter

2、actions and phosphorylation ofsignaling effectors. The MAP3Ks are highly divergent in gene numbers and structure, including TAK1, ASK1, A-Raf and C-Raf.MAPK system is a three-step sequential phosphorylation cascade which is composed of MAPK, MAP2K, and MAP3K. ERK, p38MAPK, and JNK, which are known t

3、o be activated by mechanical stimuli, belong to the MAPK family. MAP3Ks function as “platformsto integrate MAPK signaling, and activation of multiple MAP3Ks provides the spatiotemporal regulation of the MAPK pathways,which induces a wide range of physiological responses required for determining cell

4、 fate, such as cytokine production, survival,differentiation and apoptosis”.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/MAP3K.html MAP3K HYPERLINK https:/www.MedChemE/Targets/MAP3K.html HYPERLINK https:/www.MedChemE/Targets/MAP3K.html Inhibitors HYPERLINK https:/www.MedChemE/5Z-7-Oxozeaenol

5、.html 5Z-7-Oxozeaenol(FR148083; L783279; LL-Z 1640-2) Cat. No.: HY-12686 HYPERLINK https:/www.MedChemE/ask1-in-2.html ASK1-IN-2Cat. No.: HY-1319695Z-7-Oxozeaenol is a natural anti-protozoancompound from fungal origin, acting as a potentirreversible and selective inhibitor of TAK1 andVEGF-R2, with IC

6、 s of 8 nM and 52 nM,50respectively.ASK1-IN-2 is a potent and orally active inhibitorof apoptosis signal-regulating kinase 1 (ASK1),with an IC of 32.8 nM. ASK1-IN-2 can be used for50the research of ulcerative colitis.Purity: 99.50%Clinical Data: No Development ReportedSize: 1 mgPurity: 98.49%Clinica

7、l Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ask1-in-3.html ASK1-IN-3 HYPERLINK https:/www.MedChemE/ask1-in-3.html HYPERLINK https:/www.MedChemE/cot-inhibitor-1.html Cot HYPERLINK https:/www.MedChemE/cot-inhibitor-1.html HYPERLINK h

8、ttps:/www.MedChemE/cot-inhibitor-1.html inhibitor-1Cat. No.: HY-146729 Cat. No.: HY-32015ASK1-IN-3 is a potent and selective ASK1 kinaseinhibitor with IC of 33.8 nM, as well as50inhibits several cell cycle regulating kinases.ASK1-IN-3 has strong HepG2 cancer cells apoptosisinduction and potent cell

9、cycle arrest activities.Cot inhibitor-1 (compound 28) is a selectivetumor progression loci-2 (Tpl2) kinase inhibitorwith an IC of 28 nM. Cot inhibitor-1 shows an50inhibition of TNF-alpha production in human wholeblood with an IC of 5.7 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg

10、, 5 mgPurity: 98.13%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Cot-inhibitor-2.html Cot HYPERLINK https:/www.MedChemE/Cot-inhibitor-2.html HYPERLINK https:/www.MedChemE/Cot-inhibitor-2.html inhibitor-2 HYPERLINK https

11、:/www.MedChemE/Cot-inhibitor-2.html HYPERLINK https:/www.MedChemE/DLK-IN-1.html DLK-IN-1Cat. No.: HY-32018 Cat. No.: HY-114331Cot inhibitor-2 is a potent, selective and orallyactive cot (Tpl2/MAP3K8) inhibitor with anIC of 1.6 nM. Cot inhibitor-2 inhibts TNF-50production in LPS-stimulated human whol

12、e bloodwith an IC of 0.3 M.50DLK-IN-1 is a selective, orally active inhibitorof dual leucine zipper kinase (DLK, MAP3K12),with a K of 3 nM.iPurity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.41%Clinical Data: No Development Reporte

13、dSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GNE-3511.html GNE-3511 HYPERLINK https:/www.MedChemE/GNE-3511.html HYPERLINK https:/www.MedChemE/gne-8505.html GNE-8505Cat. No.: HY-12947 Cat. No.: HY-114332GNE-3511 is a dual leucine zipper kinase (DLK)inhibitor with

14、 a K of 0.5 nM.iGNE-8505 is an orally available inhibitor of Dualleucine zipper kinase (DLK).Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ASK1-IN-1.html

15、 GS-444217 HYPERLINK https:/www.MedChemE/ASK1-IN-1.html HYPERLINK https:/www.MedChemE/NG25.html NG25Cat. No.: HY-100844 Cat. No.: HY-15434GS-444217 is a potent, orally available andselective ATP-competitive inhibitor of apoptosissignal-regulating kinase 1 (ASK1) with an IC of502.87 nM.NG25 is a pote

16、nt dual TAK1 and MAP4K2inhibitor, with IC s of 149 nM and 21.7 nM,50respectively.Purity: 99.67%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.35%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-

17、228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/NQDI-1.html NQDI-1 HYPERLINK https:/www.MedChemE/NQDI-1.html HYPERLINK https:/www.MedChemE/pf-05381941.html PF-05381941Cat. No.: HY-19566 Cat. No.: HY-120823NQDI-1 inhibits apoptosis signal-regulating kinase1 (ASK1) with a Ki of 500 nM and

18、an IC50 of 3 M.PF-05381941 is a potent dual inhibitor ofTAK1/p38, with IC s of 156 and186 nM,50respectively.Purity: 95.93%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.75%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/ww

19、w.MedChemE/Selonsertib.html Selonsertib(GS-4997) Cat. No.: HY-18938 HYPERLINK https:/www.MedChemE/sm1-71.html SM1-71Cat. No.: HY-136848Selonsertib (GS-4997), an orally bioavailable,selective apoptosis signal-regulating kinase 1(ASK1) inhibitor with a pIC of 8.3, has been50evaluated as an experimenta

20、l treatment fordiabetic nephropathy and kidney fibrosis.SM1-71 (compound 5) is a potent TAK1 inhibitor,with a K of 160 nM, it also can covalentlyiinhibit MKNK2, MAP2K1/2/3/4/6/7, GAK,AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B,MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK),MAP3K1, LIMK1 and RSK2.Purity: 98.99%Cli

21、nical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 96.00%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/sw083688.html SW083688 HYPERLINK https:/www.MedChemE/sw083688.html HYPERLINK https:/www.MedChem

22、E/tak1-in-2.html TAK1-IN-2Cat. No.: HY-122232 Cat. No.: HY-132172SW083688 is a potent, highly selective TAOK2(Thousand-And-One Kinase 2) inhibitor (IC values50= 1.3 umol/L).TAK1-IN-2 is a potent and selective TAK1inhibitor, with an IC of 2 nM.50Purity: 98%Clinical Data: No Development ReportedSize:

23、1 mg, 5 mgPurity: 98.22%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/tak1-in-3.html TAK1-IN-3 HYPERLINK https:/www.MedChemE/tak1-in-3.html HYPERLINK https:/www.MedChemE/b-raf-inhibitor.html TAK1/MAP4K2 HYPERLINK https:/www.MedChemE/b-raf

24、-inhibitor.html HYPERLINK https:/www.MedChemE/b-raf-inhibitor.html inhibitor HYPERLINK https:/www.MedChemE/b-raf-inhibitor.html HYPERLINK https:/www.MedChemE/b-raf-inhibitor.html 1Cat. No.: HY-115743 Cat. No.: HY-77251TAK1-IN-3 is a potent ATP-competitive TAK1inhibitor.TAK1/MAP4K2 inhibitor 1 is a p

25、otent dualTGF-activated kinase 1 (TAK1) andmitogen-activated protein kinase kinase kinasekinase 2 (MAP4K2) inhibitor, with IC s of 41.150nM and 18.2 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL,

26、 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Takinib.html Takinib HYPERLINK https:/www.MedChemE/Takinib.html HYPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html TAO HYPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html HYPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html Kinase H

27、YPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html HYPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html HYPERLINK https:/www.MedChemE/tao-kinase-inhibitor-1.html 1(EDHS-206) Cat. No.: HY-103490 (CP 43) Cat. No.: HY-112136

28、Takinib (EDHS-206) is an orally active andselective TAK1 inhibitor (IC =9.5 nM), more than501.5 log more potent than the second and thirdranked targets, IRAK4 (120 nM) and IRAK1 (390 nM),respectively.TAO Kinase inhibitor 1 (compound 43) is aselective, ATP-competitive thousand-and-one aminoacid kinas

29、es (TAOK) inhibitor with IC s of 11 to5015 nM for TAOK1 and 2, respectively. TAO Kinaseinhibitor 1 delays mitosis and induces mitoticcell death.Purity: 99.15%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.29%Clinical Data: No Development ReportedSize: 10

30、 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/tc-ask-10.html TC HYPERLINK https:/www.MedChemE/tc-ask-10.html HYPERLINK https:/www.MedChemE/tc-ask-10.html ASK HYPERLINK https:/www.MedChemE/tc-ask-10.html HYPERLINK https:/www.MedChemE/tc-ask-10.html 10 HYPERLINK https:/www.MedChemE/tc-ask-10.html HYPERLINK https:/www.MedChemE/tpl2-kinase-inhibitor-1.html Tpl2 HYPERLINK https:/www.MedChemE/tpl2-kinase-inhibitor-1.html HYPERLINK https:/www.MedChem