Ribosomal-S6-Kinase-RSK-Inhibitors-Modulators-生命科学试剂-MedChemExpress

1、 HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html Ribosomal HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html S6 HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK

2、https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html Kinase HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html (RSK)S6KRibosomal S6 Kinase (RSK) is a family of serine/threonine protein kinases involved in th

3、e regulation of cell viability. RSK isphosphorylated in response to mitogens by activation of one or more protein kinase cascades. Phosphorylation of S6 in vivo iscatalyzed by (at least) two distinct mitogen-activated S6 kinase families distinguishable by size, the 70 kDa and 90 kDa S6 kinases.Both

4、S6 kinases are activated by serine/threonine phosphorylation.The p90 ribosomal s6 kinase family (1-4) is a group of highly conserved Ser/Thr kinases that act as downstream effectors of theRas/Raf/MEK/ERK signaling pathway. They regulate diverse cellular processes, such as cell growth, cell motility,

5、 cell survival and cellproliferation. The p70 ribosomal protein S6 kinase, an important member of AGC family, is a kind of multifunctional Ser/Thr kinases,which plays an important role in mTOR signaling cascade. The p70 ribosomal protein S6 kinase is closely associated with diversecellular processes

6、 such as protein synthesis, mRNA processing, glucose homeostasis, cell growth and apoptosis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html Ribosomal HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK https:/www.MedChemE/Targets/Ribosom

7、al S6 Kinase (RSK).html S6 HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html Kinase HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (

8、RSK).html (RSK) HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html HYPERLINK https:/www.MedChemE/Targets/Ribosomal S6 Kinase (RSK).html Inhibitors HYPERLINK https:/www.MedChemE/AD80.html AD80 HYPERLINK https:/www.MedChemE/AD80.html HYPERLINK https:/www.MedChemE/at13148.html AT13148

9、Cat. No.: HY-101963 Cat. No.: HY-16071AD80, a multikinase inhibitor, inhibits RET,RAF,SRCand S6K, with greatly reduced mTORactivity.AT13148 is an orally active and ATP-competitive,multi-AGC kinase inhibitor with IC s of 38nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM forAkt1/2/3, p70S6K, PKA, and ROCKI

10、/II, respectively.Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.42%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AT7867.html AT7867 HYPERLINK https:/www.MedChemE/AT7867.html H

11、YPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html AT7867 HYPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html HYPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html dihydrochlorideCat. No.: HY-12059 Cat. No.: HY-12059AAT7867 is a potent ATP-competitive inhibitor ofAkt1/Akt2/Akt3 and p

12、70S6K/PKA with IC s of 32nM/17 nM/47 nM and 85 nM/20 nM, respectively.AT7867 dihydrochloride is a potent ATP-competitiveinhibitor of Akt1/Akt2/Akt3 and p70S6K/PKAwith IC s of 32 nM/17 nM/47 nM and 85 nM/20 nM,respectively.Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

13、 mg, 50 mg, 100 mgPurity: 99.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BI-D1870.html BI-D1870 HYPERLINK https:/www.MedChemE/BI-D1870.html HYPERLINK https:/www.MedChemE/BIX-02565.html BIX HYPERLINK https:/www.MedChemE/BIX-02565

14、.html HYPERLINK https:/www.MedChemE/BIX-02565.html 02565Cat. No.: HY-10510 Cat. No.: HY-16104BI-D1870 is an ATP-competitive, cell permeable andbrain penetrated inhibitor of RSK isoforms, withIC s of 31 nM/24 nM/18 nM/15 nM forRSK1/RSK2/RSK3/RSK4, respectively.BIX 02565 is a potent ribosomal S6 kinas

15、e 2(RSK2) inhibitor with IC of 1.1 nM.Purity: 99.14%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mgPurity: 99.30%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/brd7389.html BRD7389 HYPERLINK http

16、s:/www.MedChemE/brd7389.html HYPERLINK https:/www.MedChemE/Carnosol.html CarnosolCat. No.: HY-12185 Cat. No.: HY-N0643BRD7389 is a specific RSK family kinase inhibitorwith IC s of 1.5 M, 2.4 M, and 1.2 M forRSK1, RSK2, and RSK3, respectively. BRD7389 isa small-molecule inducer of insulin expression

17、inpancreatic -cells.Carnosol is a potent Ribosomal S6 Kinase (RSK2)inhibitor that could be useful for treatinggastric cancer, with an IC of 5.5 M. Carnosol,a Nrf2 activator, increases the nuclear levels ofNrf2 and can promote the expression of hemeoxygenase 1 (HMOX1).Purity: 98.05%Clinical Data: No

18、Development ReportedSize: 10 mgPurity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/cki7.html CKI-7 HYPERLINK https:/www.MedChemE/cki7.html HYPERLINK https:/www.MedChemE/cki-7.html CKI-7 HYPERLINK https:/www.MedChemE/cki-7.html HYPERL

19、INK https:/www.MedChemE/cki-7.html free HYPERLINK https:/www.MedChemE/cki-7.html HYPERLINK https:/www.MedChemE/cki-7.html baseCat. No.: HY-W011109 Cat. No.: HY-133028CKI-7 is a potent and ATP-competitive casein kinase1 (CK1) IC Kiinhibitor with an of 6 M and aof 8.5 M. CKI-7 is a selective Cdc7 kina

20、seinhibitor. CKI-7 also inhibits SGK, ribosomalS6 kinase-1 (S6K1) and mitogen- andstress-activated protein kinase-1 (MSK1).CKI-7 free base is a potent and ATP-competitivecasein kinase 1 (CK1) inhibitor with an IC of 6M and a K of 8.5 M. CKI-7 free base is aselective Cdc7 kinase inhibitor.Purity: 98%

21、Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.31%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/CMK.html CMKCat. No.: HY-52101 HYPERLINK https:/www.Me

22、dChemE/eudesmin.html Eudesmin(-)-Eudesmin; Eudesmine; (-)-Eudesmine) Cat. No.: HY-N2357CMK is a RSK2 kinase inhibitor which exhibitssimilar potency but less chemical stabilitycompared with FMK.Eudesmin (-)-Eudesmin) impairs adipogenicdifferentiation via inhibition of S6K1 signalingpathway. Eudesmin

23、possesses diverse therapeuticeffects, including anti-tumor, anti-inflammatory,and anti-bacterial activities.Purity: 99.64%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mgPurity: 99.19%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/FMK.h

24、tml FMK HYPERLINK https:/www.MedChemE/FMK.html HYPERLINK https:/www.MedChemE/FMK-MEA.html FMK-MEACat. No.: HY-52101A Cat. No.: HY-52101CFMK is a an irreversible RSK2 kinase inhibitor,that covalently modifies the C-terminal kinasedomain of RSK.FMK-MEA is a potent and selective p90 RibosomalS6 Kinase

25、(RSK) inhibitor.Purity: 99.30%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/gsk-25.html GSK-25 HYPERLINK https:/www.MedChemE/gsk-25.html HYPERLINK https:/www.MedChemE/hu7

26、691.html Hu7691Cat. No.: HY-14362 Cat. No.: HY-132302GSK-25 is a potent, selective and orallybioavailable ROCK1 inhibitor (IC =7 nM). GSK-25maintains good selectivity against a panel of 31kinases (100 fold), as well as RSK1 and p70S6K(RSK1: IC =398 nM, p70S6K: IC =1 M).Hu7691 is an orally active, se

27、lective Aktinhibitor with IC s of 4.0 nM, 97.5 nM, 28 nM forAkt1, Akt2 and Akt3, respectively. Hu7691 inhibitstumor growth and enables decrease of cutaneoustoxicity in mice.Purity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Dev

28、elopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hu7691-free-base.html Hu7691 HYPERLINK https:/www.MedChemE/hu7691-free-base.html HYPERLINK https:/www.MedChemE/hu7691-free-base.html free HYPERLINK https:/www.MedChemE/hu7691-free-base.html HYPERLINK https:/www.MedChemE/hu7691-free-base

29、.html base HYPERLINK https:/www.MedChemE/hu7691-free-base.html HYPERLINK https:/www.MedChemE/LJH685.html LJH685Cat. No.: HY-132302A Cat. No.: HY-19712Hu7691 free base is an orally active, selectiveAkt inhibitor with IC s of 4.0 nM, 97.5 nM, 28nM for Akt1, Akt2 and Akt3, respectively. Hu7691free base

30、 inhibits tumor growth and enablesdecrease of cutaneous toxicity in mice.LJH685 is a potent, ATP-competitive and selectiveRSK inhibitor, inhibits RSK1, 2, and 3biochemical activities with IC s of 6, 5, 4 nM,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.99%C

31、linical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LJI308.html LJI308 HYPERLINK https:/www.MedChemE/LJI308.html HYPERLINK https:/www.MedChemE/LY-2584702-free-base.html LY-2584702 HYPERLINK https:/www.MedChemE/LY-2584702-free-base.html HYPE

32、RLINK https:/www.MedChemE/LY-2584702-free-base.html free HYPERLINK https:/www.MedChemE/LY-2584702-free-base.html HYPERLINK https:/www.MedChemE/LY-2584702-free-base.html baseCat. No.: HY-19713 Cat. No.: HY-12493LJI308 is a potent pan-ribosomal S6 kinase(RSK) inhibitor, with IC s of 6 nM, 4 nM, and 13

33、nM for RSK1, RSK2, and RSK3, respectively. LJI308inhibits the phosphorylation of RSK (T359/S363)and YB-1 (S102) after irradiation, treatment withEGF, and in cells expressing a KRAS mutation.LY-2584702 free base is a selective ATPcompetitive inhibitor of p70S6K with an IC of 4nM. In S6K1 enzyme assay

34、, the IC of LY-2584702is 2 nM.Purity: 99.21%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.56%Clinical Data: Phase 1Size: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/LY-2584702-hydrochloride.html LY-2584702 HYPERLINK https:/www.MedChemE

35、/LY-2584702-hydrochloride.html HYPERLINK https:/www.MedChemE/LY-2584702-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/LY-2584702-hydrochloride.html HYPERLINK https:/www.MedChemE/LY-2584702-tosylate-salt.html LY-2584702 HYPERLINK https:/www.MedChemE/LY-2584702-tosylate-salt.html HYPE

36、RLINK https:/www.MedChemE/LY-2584702-tosylate-salt.html tosylate HYPERLINK https:/www.MedChemE/LY-2584702-tosylate-salt.html HYPERLINK https:/www.MedChemE/LY-2584702-tosylate-salt.html saltCat. No.: HY-12493B Cat. No.: HY-12493ALY-2584702 hydrochloride is a selective ATPcompetitive inhibitor of p70S

37、6K with an IC of 4nM. In S6K1 enzyme assay, the IC of LY-2584702is 2 nM.LY-2584702 tosylate salt is a selective ATPcompetitive inhibitor of p70S6K with an IC of 4nM. In S6K1 enzyme assay, the IC of LY-2584702is 2 nM.Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mgPurity: 98.12%Clinical Data: No Dev

38、elopment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/m2698.html M2698(MSC2363318A) Cat. No.: HY-100501 HYPERLINK https:/www.MedChemE/mbm-55s.html MBM-55SCat. No.: HY-101029AM2698 (MSC2363318A) is an orally active, ATPcompetitive, selective p70S6K and Aktdual-in

39、hibitor with IC s of 1 nM for p70S6K, Akt1and Akt3. M2698 can cross the blood-brain barrierand has anti-cancer activity.MBM-55S is a potent NIMA-related kinase 2(Nek2) inhibitor with an IC of 1 nM. MBM-55Sshows a 20-fold or greater selectivity in mostkinases with the exception of RSK1 (IC =5.4 nM)an

40、d DYRK1a (IC =6.5 nM).Purity: 99.74%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/PF-4708671.html PF-4708671Cat. No.: HY-15773 HYPERLINK https:/www.MedChemE/Pluripotin.html Pluripotin(SC1) Cat. No.: HY-

41、10579PF-4708671 is a potent cell-permeable S6K1inhibitor with a Ki of 20 nM and IC of 160 nM.Pluripotin is a dual inhibitor of ERK1 andRasGAPwith K s of 98 nM and 212 nM,respectively. Pluripotin also inhibits RSK1,RSK2, RSK3, and RSK4 with IC s of 0.5, 2.5,3.3, and 10.0 M, respectively.Purity: 99.94

42、%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.86%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/Quercitrin.html Quercitrin HYPERLINK https:/www.MedChemE/Quercitrin.html HYP

43、ERLINK https:/www.MedChemE/rsk-in-1.html RSK-IN-1(Quercetin 3-rhamnoside) Cat. No.: HY-N0418Cat. No.: HY-144434Quercitrin is a natural compound found in Tartarybuckwheat with a potential anti-inflammationeffect that is used to treat heart and vascularconditions.RSK-IN-1 (compound 7d) is a RSK inhibi

44、tor thatinhibits the YB-1 phosphorylation. RSK-IN-1 hasanti-tumor effects.Purity: 99.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rsk4-in-1.html RSK4-IN-1 HYPERLINK https:/www.MedChemE/rsk4-in-1.html HYPERLINK https:/www.MedChemE/SL_0101-1.html SL HYPERLINK https:/www.MedChemE/SL_0101-1.html HYPERLINK https:/www.MedChemE/SL_0101-1.html 0101-1Cat. No.: HY-132891(SL0101) Cat. No