IRAK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/IRAK.html IRAKInterleukin-1 receptor associated kinase; IL-1R associated kinaseInterleukin-1 receptor-associated kinases (IRAKs), are serine/threonine kinases, play critical roles in initiating innate immuneresponses against foreign pathogens and other types of

2、 dangers through their role in Toll-like receptor (TLR) and interleukin 1receptor (IL-1R) mediated signaling pathways. The four different IRAK-like molecules have been identified: two active kinases,IRAK-1 and IRAK-4, and two inactive kinases, IRAK-2 and IRAK-M. All IRAKs mediate activation of nucle

3、ar factor-kappaB (NF-B)and mitogen-activated protein kinase (MAPK) pathways.Toll-like receptors transduce their signals through the adaptor molecule MyD88 and members of the IL-1R-associated kinase family(IRAK-1, 2, M and 4). IRAK-1 and IRAK-2, known to form Myddosomes with MyD88-IRAK-4, mediate TLR

4、7-induced TAK1-dependentNF-B activation. IRAK-M is known to function as a negative regulator that prevents the dissociation of IRAKs from MyD88, therebyinhibiting downstream signalling.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/IRAK.html IRAK HYPERLINK https:/www.MedChemE/Targets/IRAK.html

5、 HYPERLINK https:/www.MedChemE/Targets/IRAK.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/IRAK.html HYPERLINK https:/www.MedChemE/Targets/IRAK.html & HYPERLINK https:/www.MedChemE/Targets/IRAK.html HYPERLINK https:/www.MedChemE/Targets/IRAK.html Modulators HYPERLINK https:/www.MedChemE/as244

6、4697.html AS2444697 HYPERLINK https:/www.MedChemE/as2444697.html HYPERLINK https:/www.MedChemE/AZ1495.html AZ1495Cat. No.: HY-18992 Cat. No.: HY-111101AS2444697 is an orally active IRAK-4 inhibitor withan IC of 21 nM. AS2444697 potently inhibits50human and rat IRAK-4 activity. AS2444697 exhibitsreno

7、protective effects through anti-inflammatoryaction.AZ1495 (compound 28) is an oral active inhibitorof Interleukin-1 receptor associated kinase 4(IRAK4), with IC values of 5 nM and 23 nM for50IRAK4 and IRAK1, respectively. Shows activity intreatment of mutant MYD88L265P diffuse largeB-cell lymphoma (

8、DLBCL).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.18%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ca-4948-1.html CA-4948Cat. No.: HY-135317 HYPERLINK https:/www.MedChemE/Ginsenoside-Rb1.html G

9、insenoside HYPERLINK https:/www.MedChemE/Ginsenoside-Rb1.html HYPERLINK https:/www.MedChemE/Ginsenoside-Rb1.html Rb1(Gypenoside III) Cat. No.: HY-N0039CA-4948 is a potent IRAK4/FLT3 inhibtor withanti-tumor activity.Ginsenoside Rb1, a main constituent of the root ofPanax ginseng, inhibits Na+, K+-ATP

10、aseactivity with an IC of 6.31.0 M. Ginsenoside50also inhibits IRAK-1 activation and phosphorylationof NF-B p65 .Purity: 99.96%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100

11、 mg HYPERLINK https:/www.MedChemE/hg-12-6.html HG-12-6 HYPERLINK https:/www.MedChemE/hg-12-6.html HYPERLINK https:/www.MedChemE/hs271.html HS271Cat. No.: HY-123956 Cat. No.: HY-131903HG-12-6 is a type II inhibitor of IRAK4. HG-12-6shows preferential binding to unphosphorylatedinactive IRAK4 with an

12、IC of 165 nM. HG-12-6 can50modulate IRAK4 activity in autoimmunity andinflammation.HS271 is a highly potent, orally active andselective IRAK4 inhibitor, with an IC of 7.2 M.50HS271 exhibits superior enzymatic and cellularactivities, as well as excellent pharmacokineticproperties.Purity: 98%Clinical

13、Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/IRAK-inhibitor-1.html IRAK HYPERLINK https:/www.MedChemE/IRAK-inhibitor-1.html HYPERLINK https:/www.MedChemE/IRAK-inhibit

14、or-1.html inhibitor HYPERLINK https:/www.MedChemE/IRAK-inhibitor-1.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-1.html 1 HYPERLINK https:/www.MedChemE/IRAK-inhibitor-1.html HYPERLINK https:/www.MedChemE/irak-inhibitor-2.html IRAK HYPERLINK https:/www.MedChemE/irak-inhibitor-2.html HYPERLINK htt

15、ps:/www.MedChemE/irak-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/irak-inhibitor-2.html HYPERLINK https:/www.MedChemE/irak-inhibitor-2.html 2Cat. No.: HY-13275 Cat. No.: HY-13276IRAK inhibitor 1 is a potent IRAK-4 inhibitor withIC of 216 nM, is poorly active against JNK-1 and50JNK-2 wit

16、h IC of 3.801 M, and 10 M,50respectively.IRAK inhibitor 2 is interleukin-1 receptorassociated kinase inhibitor .Purity: 98.05%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.87%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK h

17、ttps:/www.MedChemE/IRAK-inhibitor-3.html IRAK HYPERLINK https:/www.MedChemE/IRAK-inhibitor-3.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-3.html inhibitor HYPERLINK https:/www.MedChemE/IRAK-inhibitor-3.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-3.html 3 HYPERLINK https:/www.MedChemE/IRAK

18、-inhibitor-3.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4.html IRAK HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4.html inhibitor HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4.html 4Cat. N

19、o.: HY-13277 Cat. No.: HY-13278IRAK inhibitor 3 is an interleukin-1 (IL-I)receptor-associated kinase (IRAK) kinase modulatorextracted from patent WO2008030579 A2.IRAK inhibitor 4 is an interleukin-1 receptorassociated kinase 4(IRAK4) inhibitor.Purity: 98.17%Clinical Data: No Development ReportedSize

20、: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4-trans.html IRAK HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4-trans.html HYPERLINK https:/www.MedCh

21、emE/IRAK-inhibitor-4-trans.html inhibitor HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4-trans.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4-trans.html 4 HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4-trans.html HYPERLINK https:/www.MedChemE/IRAK-inhibitor-4-trans.html trans HYPERLINK https:/w

22、ww.MedChemE/IRAK-inhibitor-4-trans.html HYPERLINK https:/www.MedChemE/irak-inhibitor-6.html IRAK HYPERLINK https:/www.MedChemE/irak-inhibitor-6.html HYPERLINK https:/www.MedChemE/irak-inhibitor-6.html inhibitor HYPERLINK https:/www.MedChemE/irak-inhibitor-6.html HYPERLINK https:/www.MedChemE/irak-in

23、hibitor-6.html 6Cat. No.: HY-13278A Cat. No.: HY-13280IRAK inhibitor 4 (trans) is the trans form of IRAKinhibitor 4. IRAK inhibitor 4 is an interleukin-1receptor associated kinase 4 (IRAK4) inhibitor.IRAK inhibitor 6 is an inhibitor of interleukin-1receptor associated kinase 4 (IRAK-4) with IC of501

24、60 nM.Purity: 99.09%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/IRAK-1-4-Inhibitor-I.html IRAK-1-4 HYPERLINK https:/www.MedChemE/IRAK-1-4-Inhibitor-I.html HYPERLINK https:/www.M

25、edChemE/IRAK-1-4-Inhibitor-I.html Inhibitor HYPERLINK https:/www.MedChemE/IRAK-1-4-Inhibitor-I.html HYPERLINK https:/www.MedChemE/IRAK-1-4-Inhibitor-I.html I(IRAK-1/4 Inhibitor I) Cat. No.: HY-13329 HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html IRAK-4 HYPERLINK https:/www.MedC

26、hemE/irak-4-protein-kinase-inhibitor-2.html HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html protein HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html kinase HYPERLINK https:/www.MedChemE/irak

27、-4-protein-kinase-inhibitor-2.html HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html HYPERLINK https:/www.MedChemE/irak-4-protein-kinase-inhibitor-2.html 2Cat. No.: HY-77048IRAK-1-4 Inhibitor I is an in

28、hibitor ofinterleukin-1 receptor-associated kinase 1/4 (IRAK1/4) with IC s of 0.2 M and 0.3 M,50respectively.IRAK-4 protein kinase inhibitor 2 (compound 1) isa potent inhibitor of interleukin-1 (IL-1)receptor-associated kinase-4 (IRAK-4), with an ICof 4 M. IRAK-4 protein kinase inhibitor 2 can beuse

29、d for the research of inflammatory andimmune-related conditions or disorders.50Purity: 99.88%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg HYPERLINK https:/www.MedChemE/IRAK4-IN-1.html IRAK4-IN-1 HYPE

30、RLINK https:/www.MedChemE/IRAK4-IN-1.html HYPERLINK https:/www.MedChemE/irak4-in-4-1.html IRAK4-IN-4Cat. No.: HY-101922 Cat. No.: HY-114181IRAK4-IN-1 is an interleukin-1 receptor associatedkinase 4 (IRAK4) inhibitor with an IC of 7 nM.50IRAK4-IN-4 is an interleukin-1 receptor-associatedkinase 4 (IRA

31、K4) inhibitor extracted from patentCN107163044A, Compound15, has an IC of 2.8 nM.50IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase(cGAS) with an IC of 2.1 nM.50Purity: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.72%Clinical Data: No

32、 Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/irak4-in-6.html IRAK4-IN-6 HYPERLINK https:/www.MedChemE/irak4-in-6.html HYPERLINK https:/www.MedChemE/CA-4948.html IRAK4-IN-7Cat. No.: HY-130253 Cat. No.: HY-109585IRAK4-IN-6 is an orally efficaci

33、ous and selectiveIRAK4 inhibitor with an IC of 4 nM, and targetes50MyD88 L265P mutant diffuse large B cell lymphoma.IRAK4-IN-7 is a selective, potent and orallyactive interleukin-1 receptor-associated kinase 4(IRAK4) inhibitor, extracted from patentWO2015104688 (example 1). IRAK4-IN-7 has thepotenti

34、al for cancer and inflammatory diseasestreatment.Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.86%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/irak4-in-8.html IRAK4-IN-8 HYPERLINK

35、https:/www.MedChemE/irak4-in-8.html HYPERLINK https:/www.MedChemE/jh-x-119-01.html JH-X-119-01Cat. No.: HY-143231 Cat. No.: HY-103017AIRAK4-IN-8 (VI-177) is a potent IRAK4 inhibitor.JH-X-119-01 is a potent and selectiveinterleukin-1 receptor-associated kinases 1 (IRAK1)inhibitor. JH-X-119-01 amelior

36、ates LPS-inducedsepsis in mice.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/JH-X-119-01_hydrochloride.html JH-X-119-01 HYPERLINK https:/www.MedCh

37、emE/JH-X-119-01_hydrochloride.html HYPERLINK https:/www.MedChemE/JH-X-119-01_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/JH-X-119-01_hydrochloride.html HYPERLINK https:/www.MedChemE/pf-06426779.html PF-06426779Cat. No.: HY-103017 Cat. No.: HY-123854JH-X-119-01 hydrochloride is a p

38、otent andselective interleukin-1 receptor-associatedkinases 1 (IRAK1) inhibitor. JH-X-119-01hydrochloride ameliorates LPS-induced sepsis inmice.PF-06426779 is a potent and selective inhibitor ofinterleukin1 receptor associated kinase 4 (IRAK4),with an IC of 0.3 nM.50Purity: 89.79%Clinical Data: No D

39、evelopment ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mgPurity: 99.83%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/protac-irak4-degrader-1.html PROTAC HYPERLINK https:/www.MedChemE/protac-irak4-degrader-1.html HYPERLINK https:/www.MedChemE/

40、protac-irak4-degrader-1.html IRAK4 HYPERLINK https:/www.MedChemE/protac-irak4-degrader-1.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-1.html degrader-1 HYPERLINK https:/www.MedChemE/protac-irak4-degrader-1.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-3.html PROTAC HYPERLINK h

41、ttps:/www.MedChemE/protac-irak4-degrader-3.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-3.html IRAK4 HYPERLINK https:/www.MedChemE/protac-irak4-degrader-3.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-3.html degrader-3Cat. No.: HY-129966 Cat. No.: HY-135382APROTAC IRAK4 degrad

42、er-1 is a Cereblon-based PROTACinterleukin-1 receptor-associated kinase 4 (IRAK4)degrader extracted from patent US20190192668A1Compound I-210, makes 20-50%, and50% IRAK4 degradation at 0.01, 0.1, and 1 Min OCI-LY-10 cells, respectively.PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4degrader based

43、on von Hippel-Lindau.Purity: 99.55%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/protac-irak4-degrader-4.html PROTAC HYPERLINK https:/www.MedChemE/protac-irak4-degrader-4.ht

44、ml HYPERLINK https:/www.MedChemE/protac-irak4-degrader-4.html IRAK4 HYPERLINK https:/www.MedChemE/protac-irak4-degrader-4.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-4.html degrader-4 HYPERLINK https:/www.MedChemE/protac-irak4-degrader-4.html HYPERLINK https:/www.MedChemE/protac-irak4-d

45、egrader-5.html PROTAC HYPERLINK https:/www.MedChemE/protac-irak4-degrader-5.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-5.html IRAK4 HYPERLINK https:/www.MedChemE/protac-irak4-degrader-5.html HYPERLINK https:/www.MedChemE/protac-irak4-degrader-5.html degrader-5Cat. No.: HY-139315 Cat. N

46、o.: HY-139316PROTAC IRAK4 degrader-4 is a Cereblon-based PROTACas interleukin-1 receptor-associated kinase 4(IRAK4) degrader extracted from patentUS20190192668A1, compound I-127.PROTAC IRAK4 degrader-5 is a Cereblon-based IRAK4degrader extracted from patent US20190192668A1,compound I-171.Purity: 98%Clinic