IKK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/IKK.html IKKIB kinase; I kappa B kinaseIKK is a complex composed of three subunits: IKK, IKK, and IKK (also called NEMO). The complex is the signal integration hubfor NF-B activation. It integrates signals from all NF-B activating stimuli to catalyze the phosph

2、orylation of various IB and NF-Bproteins, as well as of other substrates. The human IKK family has four members, the IKKs IKK-alpha and IKK-beta, and theIKK-related kinases TBK1 and IKK-epsilon.Two members, IKK and IKK, the so-called canonical members, phosphoryate IB, leading to activation of the t

3、ranscription factorNF-B, which controls the expression of many immune and inflammatory genes. The IKK-related proteins TBK-1 and IKK-epsilonhave a different substrate-IRF3-which regulates a different set of genes, the products of which include Type I interferons. IKKs area therapeutic target due to

4、their crucial roles in various biological processes, including the immune response, the stress response,and tumor development.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/IKK.html IKK HYPERLINK https:/www.MedChemE/Targets/IKK.html HYPERLINK https:/www.MedChemE/Targets/IKK.html Inhibitors HYP

5、ERLINK https:/www.MedChemE/rac-bay-985.html (Rac)-BAY-985Cat. No.: HY-133117A HYPERLINK https:/www.MedChemE/ACHP-Hydrochloride.html ACHP HYPERLINK https:/www.MedChemE/ACHP-Hydrochloride.html HYPERLINK https:/www.MedChemE/ACHP-Hydrochloride.html Hydrochloride(IKK-2 Inhibitor VIII) Cat. No.: HY-13060(

6、Rac)-BAY-985 (Compound Example 100.01) is apotent, ATP-competitive and selective TBK1inhibitor with an IC of 1.5 nM. Antitumor50efficacy.ACHP Hydrochloride (IKK-2 Inhibitor VIII) is ahighly potent and selective IKK- inhibitor with anIC of 8.5 nM.50Purity: 98%Clinical Data: No Development ReportedSiz

7、e: 1 mg, 5 mgPurity: 99.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Amlexanox.html Amlexanox(AA673; Amoxanox; CHX3673) Cat. No.: HY-B0713 HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-6.html Anti-inflammatory HYPERLINK h

8、ttps:/www.MedChemE/anti-inflammatory-agent-6.html HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-6.html agent HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-6.html HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-6.html 6Cat. No.: HY-139833Amlexanox (AA673; Amoxanox; CHX3673) is a

9、 specificinhibitor of IKK and TBK1, and inhibits the IKKand TBK1 activity determined by MBPphosphorylation with an IC of approximately 1-250M.Anti-inflammatory agent 6 blocks thephosphorylation of I kappa b kinase / (IKK/),IB, and nuclear factor kB p65 (NF-B p65) whichis a key controller of inflamma

10、tion, therebyshowing anti-inflammatory potential.Purity: 99.88%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZD3264.html AZD3264Cat. No.: HY-19362 HYPERLINK https:/www.MedChemE/BAY-11-7082

11、.html BAY HYPERLINK https:/www.MedChemE/BAY-11-7082.html HYPERLINK https:/www.MedChemE/BAY-11-7082.html 11-7082(BAY 11-7821) Cat. No.: HY-13453AZD3264 is a selective IkB-kinase IKK2 inhibitor.BAY 11-7082 is an IB phosphorylation and NF-Binhibitor. BAY 11-7082 selectively andirreversibly inhibits the

12、 TNF-inducedphosphorylation of IB-, and decreases NF-B andexpression of adhesion molecules.Purity: 99.67%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK

13、https:/www.MedChemE/Bay-65-1942-R-form.html Bay HYPERLINK https:/www.MedChemE/Bay-65-1942-R-form.html HYPERLINK https:/www.MedChemE/Bay-65-1942-R-form.html 65-1942 HYPERLINK https:/www.MedChemE/Bay-65-1942-R-form.html HYPERLINK https:/www.MedChemE/Bay-65-1942-R-form.html (R HYPERLINK https:/www.MedC

14、hemE/Bay-65-1942-R-form.html HYPERLINK https:/www.MedChemE/Bay-65-1942-R-form.html form) HYPERLINK https:/www.MedChemE/Bay-65-1942-R-form.html HYPERLINK https:/www.MedChemE/bay-65-1942-free-base.html Bay HYPERLINK https:/www.MedChemE/bay-65-1942-free-base.html HYPERLINK https:/www.MedChemE/bay-65-19

15、42-free-base.html 65-1942 HYPERLINK https:/www.MedChemE/bay-65-1942-free-base.html HYPERLINK https:/www.MedChemE/bay-65-1942-free-base.html free HYPERLINK https:/www.MedChemE/bay-65-1942-free-base.html HYPERLINK https:/www.MedChemE/bay-65-1942-free-base.html baseCat. No.: HY-50949A Cat. No.: HY-5094

16、9Bay 65-1942 R form is the less active R-form ofBay 65-1942. Bay 65-1942 is an ATP-competitive andselective IKK inhibitor.Bay 65-1942 free base is an ATP-competitive andselective IKK inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development Reporte

17、dSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Bay-65-1942-hydrochloride.html Bay HYPERLINK https:/www.MedChemE/Bay-65-1942-hydrochloride.html HYPERLINK https:/www.MedChemE/Bay-65-1942-hydrochloride.html 65-1942 HYPERLINK https:/www.MedChemE/Bay-65-1942-hydrochloride.html HYPERLINK https:/www.MedCh

18、emE/Bay-65-1942-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Bay-65-1942-hydrochloride.html HYPERLINK https:/www.MedChemE/bay-985.html BAY-985Cat. No.: HY-50948 Cat. No.: HY-133117Bay 65-1942 hydrochloride is an ATP-competitiveand selective IKK inhibitor.BAY-985 is a highly potent,

19、 orally active andselective ATP-competitive dual inhibitor of TBK1and IKK with IC s of 2/30 and 2 nM for TBK150(low/high ATP) and IKK, respectively. Antitumorefficacy.Purity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mgPurity: 99.87%Clinical Data: No Development Re

20、portedSize: 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/BI605906.html BI605906 HYPERLINK https:/www.MedChemE/BI605906.html HYPERLINK https:/www.MedChemE/BMS-066.html BMS-066Cat. No.: HY-13019 Cat. No.: HY-18710

21、BI605906 is a novel IKK inhibitor with an IC50value of 380 nM when assayed at 0.1 mM ATP.BMS-066 is an IKK/Tyk2 pseudokinase inhibitor,with IC s of 9 nM and 72 nM, respectively.50Purity: 99.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Deve

22、lopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/BMS-345541-free-base.html BMS-345541 HYPERLINK https:/www.MedChemE/BMS-345541-free-base.html HYPERLINK https:/www.MedChemE/BMS-345541.html BMS-345541 HYPERLINK https:/www.MedChemE/BMS-345541.html HYPERLINK https:/www.MedChemE/BMS-345541.

23、html hydrochlorideCat. No.: HY-10519 Cat. No.: HY-10518BMS-345541 is a selective inhibitor of thecatalytic subunits of IKK (IKK-2 IC50=0.3 M, IKK-1IC =4 M). BMS-345541 binds at an allosteric site50of IKK.BMS-345541 hydrochloride is a selective inhibitorof the catalytic subunits of IKK (IKK-2 IC =0.3

24、 M,50IKK-1 IC =4 M). BMS-345541 binds at an allosteric50site of IKK.Purity: 99.57%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BX795.html

25、 BX795 HYPERLINK https:/www.MedChemE/BX795.html HYPERLINK https:/www.MedChemE/chicanine.html ChicanineCat. No.: HY-10514 Cat. No.: HY-N2270BX795 is a potent and selective inhibitor ofPDK1, with an IC of 6 nM. BX795 is also a50potent and relatively specific inhibitor of TBK1and IKK, with an IC of 6 a

26、nd 41 nM,50respectively.Chicanine is a lignan compound of Schisandrachinesis, inhibits LPS-induced phosphorylation ofp38 MAPK, ERK 1/2 and IB-, withanti-inflammatory activity.Purity: 99.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mgPurity: 98%Cli

27、nical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Ertiprotafib.html Ertiprotafib HYPERLINK https:/www.MedChemE/Ertiprotafib.html HYPERLINK https:/www.MedChemE/glabrescone-c.html Glabrescone HYPERLINK https:/www.MedChemE/glabrescone-c.html HYPERLINK https:/www.MedChem

28、E/glabrescone-c.html C(PTP 112) Cat. No.: HY-19383Cat. No.: HY-N10112Ertiprotafib is an inhibitor of PTP1B, IkB kinase (IKK-), and a dual PPAR and PPAR agonist,with an IC of 1.6 M for PTP1B, 400 nM for50IKK-, an EC of 1 M for PPAR/PPAR.50Glabrescone C possesses potent anti-inflammatoryactivity by di

29、rectly bnding to IKK/.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/gs143.html GS143 HYPERLINK https:/www.MedChemE/gs143.html HYPERLINK https:/www.MedChemE/ikk-3-inhibitor.html

30、GSK319347ACat. No.: HY-110261 Cat. No.: HY-14682GS143 is a selective IB ubiquitination inhibitorwith an IC of 5.2 M for SCFTrCP1-mediated50IB ubiquitylation. GS143 suppresses NF-Bactivation and transcription of target genesand does not inhibit proteasome activity. GS143has anti-asthma effect.GSK3193

31、47A is a dual inhibitor of TBK1 and IKKwith IC s of 93 nM and 469 nM, respectively.50GSK319347A also inhibits IKK2 with an IC of 79050nM.Purity: 98.30%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.93%Clinical Data: No Development ReportedSize: 10

32、 mM 1 mL, 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/gsk8612.html GSK8612Cat. No.: HY-111941 HYPERLINK https:/www.MedChemE/hoipin-1.html HOIPIN-1(JTP-0819958) Cat. No.: HY-122881GSK8612 is a highly selective and potentTank-binding Kinase-1 (TBK1) inhibitor, with apIC of 6.8 for recombina

33、nt TBK1.50HOIPIN-1 (JTP-0819958) is a selective linearubiquitin chain assembly complex (LUBAC)inhibitor with an IC of 2.8 M. HOIPIN-150suppress LUBAC-mediated NF-kB activation in vitro.Purity: 99.33%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 97.1

34、0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/hpn-01.html HPN-01 HYPERLINK https:/www.MedChemE/hpn-01.html HYPERLINK https:/www.MedChemE/IKK-16.html IKK HYPERLINK https:/www.MedChemE/IKK-16.html HYPERLINK https:/www.MedChemE/IKK-16.html

35、 16Cat. No.: HY-135366 Cat. No.: HY-13687HPN-01 is a potent and selective IKK inhibitor,with pIC values of 6.4, 7.0 and 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/IKK-IN-1.html IKK-IN-1 HYPE

36、RLINK https:/www.MedChemE/IKK-IN-1.html HYPERLINK https:/www.MedChemE/IMD-0354.html IMD-0354Cat. No.: HY-146723(IKK2 Inhibitor V) Cat. No.: HY-10172IKK-IN-1 is a potent and orally active IkappaB(IKK-) inhibitor with IC of 0.20 M. IKK-IN-150can reduce PGE2 and TNF- production in mousemacrophage cells

37、. IKK-IN-1 has the ability toprotect mice against septic shock inducedmortality.IMD-0354 (IKK2 Inhibitor V) is a selective IKKinhibitor which inhibits NF-B activity. IMD0354inhibits TNF- induced NF-B transcriptionactivity with an IC of 1.2 uM.50Purity: 98%Clinical Data: No Development ReportedSize:

38、1 mg, 5 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/IMD-0560.html IMD-0560 HYPERLINK https:/www.MedChemE/IMD-0560.html HYPERLINK https:/www.MedChemE/INH14.html INH14

39、Cat. No.: HY-105661 Cat. No.: HY-114454IMD-0560 is a novel IB kinase inhibitor.INH14 is a cell permeable inhibitor of IKK/IKK,with IC s of 8.97 and 3.59 M, respectively.50INH14 inhibits the IKK/-dependent TLRinflammatory response. INH14 also inhibitsdownstream of TAK1/TAB1 and NF-kB pathways.Anti-in

40、flammatory and anti-cancer activity.Purity: 99.67%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, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LY2409881.html LY2409881 HYP

41、ERLINK https:/www.MedChemE/LY2409881.html HYPERLINK https:/www.MedChemE/LY2409881-trihydrochloride.html LY2409881 HYPERLINK https:/www.MedChemE/LY2409881-trihydrochloride.html HYPERLINK https:/www.MedChemE/LY2409881-trihydrochloride.html trihydrochlorideCat. No.: HY-B0788 Cat. No.: HY-B0788ALY240988

42、1 is a selective IB kinase (IKK2)inhibitor with an IC of 30 nM.50LY2409881 trihydrochloride is a selective IBkinase (IKK2) inhibitor with an IC of 30 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.92%Clinical Data: No Development ReportedSize: 10 mM

43、1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/malachite-green-oxalate.html Malachite HYPERLINK https:/www.MedChemE/malachite-green-oxalate.html HYPERLINK https:/www.MedChemE/malachite-green-oxalate.html green HYPERLINK https:/www.MedChemE/malachite-green-oxalate.html HYPERLINK https

44、:/www.MedChemE/malachite-green-oxalate.html oxalateCat. No.: HY-D0162 HYPERLINK https:/www.MedChemE/MLN120B.html MLN120B(ML120B) Cat. No.: HY-15473Malachite green oxalate is a triphenylmethane dyewhich can be used to detect the release ofphosphate in enzymatic reactions. Malachite greenoxalate is al

45、so a potent and selective inhibitorof IKBKE, and inhibits its downstream targets suchas IB, p65 and IRF3.MLN120B (ML120B) is a potent, ATP competitive, andorally active inhibitor of IKK withan IC of 60 nM. MLN120B inhibits50multiple myeloma cell growth in vitro and in vivoand also can be used for th

46、e research ofrheumatoid arthritis.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mgPurity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/mln120b-dihydrochloride.html MLN120B HYPERLINK https:/www.MedChemE/mln12

47、0b-dihydrochloride.html HYPERLINK https:/www.MedChemE/mln120b-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/mln120b-dihydrochloride.html HYPERLINK https:/www.MedChemE/MRT67307.html MRT67307(ML120B dihydrochloride) Cat. No.: HY-15473ACat. No.: HY-13018MLN120B dihydrochloride (ML1

48、20B dihydrochloride)is a potent, ATP competitive, and orally activeinhibitor of IKK with an IC of 60 nM.50MLN120B inhibits multiple myeloma cell growth invitro and in vivo and also can be used for theresearch of rheumatoid arthritis.MRT67307 is a dual inhibitor of the IKK and TBK-1with IC s of 160 a

49、nd 19 nM, respectively.50MRT67307 also inhibits ULK1 and ULK2 with IC s50of 45 and 38 nM, respectively. MRT67307 alsoblocks autophagy in cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.34%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 10

50、0 mg HYPERLINK https:/www.MedChemE/mrt67307-hydrochloride.html MRT67307 HYPERLINK https:/www.MedChemE/mrt67307-hydrochloride.html HYPERLINK https:/www.MedChemE/mrt67307-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/mrt67307-hydrochloride.html HYPERLINK https:/www.MedChemE/nf-b-in-1.

51、html NF-B-IN-1Cat. No.: HY-13018A Cat. No.: HY-138537MRT67307 hydrochloride is a dual inhibitor of theIKK and TBK-1 with IC s of 160 and 19 nM,50respectively. MRT67307 hydrochloride also inhibitsULK1 and ULK2 with IC s of 45 and 38 nM,50respectively. MRT67307 hydrochloride also blocksautophagy in ce

52、lls.NF-B-IN-1, a 4-arylidene crucumin analogue, is apotent NF-B signaling pathway inhibitor.NF-B-IN-1 directly inhibits IKK to block NF-Bactivation. NF-B-IN-1 effectively inhibits theviability of lung cancer cells and attenuates theclonogenic activity of A549 cells.Purity: 98%Clinical Data: No Devel

53、opment ReportedSize: 1 mg, 5 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/pf-184.html PF-184 HYPERLINK https:/www.MedChemE/pf-184.html HYPERLINK https:/www.MedChemE/pha-408.html PHA HYPERLINK htt

54、ps:/www.MedChemE/pha-408.html HYPERLINK https:/www.MedChemE/pha-408.html 408Cat. No.: HY-107591 Cat. No.: HY-14180PF-184 is a potent inhibitory factor-B kinase 2(IKK-2) inhibitor with an IC of 37 nM. PF-184 has50anti-inflammatory effects.PHA 408 (PHA-408) is a potent, selective andorally active IB k

55、inase-2 (IKK-2) inhibitor. PHA408 is a powerful anti-inflammatory agent againstlipopolysaccharide (LPS)- and cigarette smoke(CS)-mediated lung inflammation.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK htt

56、ps:/www.MedChemE/plantainoside-d.html Plantainoside HYPERLINK https:/www.MedChemE/plantainoside-d.html HYPERLINK https:/www.MedChemE/plantainoside-d.html D HYPERLINK https:/www.MedChemE/plantainoside-d.html HYPERLINK https:/www.MedChemE/PS-1145.html PS-1145Cat. No.: HY-N5063 Cat. No.: HY-18008Planta

57、inoside D shows ACE inhibitory activitywith IC 2.17 mM. And plantainoside D is a50promising IKK- inhibitor.PS-1145 is an IB kinase (IKK) inhibitor with anIC of 88 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.88%Clinical Data: No Development ReportedSize: 1

58、0 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Resveratrol.html Resveratrol(trans-Resveratrol; SRT501) Cat. No.: HY-16561 HYPERLINK https:/www.MedChemE/resveratrol-analog-1.html Resveratrol HYPERLINK https:/www.MedChemE/resveratrol-analog-1.html HYPERLINK https:/www.MedCh

59、emE/resveratrol-analog-1.html analog HYPERLINK https:/www.MedChemE/resveratrol-analog-1.html HYPERLINK https:/www.MedChemE/resveratrol-analog-1.html 1Cat. No.: HY-136203Resveratrol (trans-Resveratrol; SRT501), a naturalpolyphenolic phytoalexin that possessesanti-oxidant, anti-inflammatory, cardiopro

60、tective,and anti-cancer properties.Resveratrol analog 1 is an analog of Resveratrol(HY-16561), compound 48. Resveratrol is anatural polyphenolic phytoalexin that possessesanti-oxidant, anti-inflammatory, cardioprotective,and anti-cancer properties.Purity: 99.89%Clinical Data: LaunchedSize: 10 mM 1 m