Akt-Inhibitors-Modulators-生命科学试剂-MedChemExpress

1、 HYPERLINK https:/www.MedChemE/Targets/Akt.html AktPKB; Protein kinase BAkt/PKB (Protein kinase B), a serine/threonine protein kinase with antiapoptotic activity, is one of the major downstream targets ofPtdIns(3,4,5)P3 signaling pathway. It contains a pleckstrin homology domain (PH domain) that spe

2、cifically binds PtdIns(3,4,5)P3 onthe plasma membrane. Akt phosphorylation and activation are directly determined by the level of PtdIns(3,4,5)P3 on the plasmamembrane, which is regulated by PI3K.Akt consists of three isoforms: PKB/Akt1, PKB/Akt2 and PKB/Akt3. Akt isoforms have an N-terminal PH (ple

3、ckstrin homology)domain and a kinase domain, which are separated by a 39-amino-acid hinge region. Catalytically active Akt regulates the functionof numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis.Akt is a crucial mediator of cell survival and it

4、s deactivation is implicated in various stress-induced pathological cell death anddegenerative diseases.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Akt.html Akt HYPERLINK https:/www.MedChemE/Targets/Akt.html HYPERLINK https:/www.MedChemE/Targets/Akt.html Inhibitors, HYPERLINK https:/www.Med

5、ChemE/Targets/Akt.html HYPERLINK https:/www.MedChemE/Targets/Akt.html Activators HYPERLINK https:/www.MedChemE/Targets/Akt.html HYPERLINK https:/www.MedChemE/Targets/Akt.html & HYPERLINK https:/www.MedChemE/Targets/Akt.html HYPERLINK https:/www.MedChemE/Targets/Akt.html Modulators HYPERLINK https:/w

6、ww.MedChemE/e-akt-inhibitor-iv.html (E)-Akt HYPERLINK https:/www.MedChemE/e-akt-inhibitor-iv.html HYPERLINK https:/www.MedChemE/e-akt-inhibitor-iv.html inhibitor-IV(E)-AKTIV) Cat. No.: HY-14971 HYPERLINK https:/www.MedChemE/z-guggulsterone.html (Z)-GuggulsteroneCat. No.: HY-110066(E)-Akt inhibitor-I

7、V (E)-AKTIV) is a PI3K-Aktinhibitor, with potent cytotoxic.Z-guggulsterone, a constituent of Indian Ayurvedicmedicinal plant Commiphora mukul, inhibitsthe growth of human prostate cancer cells bycausing apoptosis. Z-guggulsterone inhibitsangiogenesis by suppressing the VEGFVEGF-R2Aktsignaling axis.P

8、urity: 98.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/1,3-Dicaffeoylquinic-acid.html 1,3-Dicaffeoylquinic HYPERLINK ht

9、tps:/www.MedChemE/1,3-Dicaffeoylquinic-acid.html HYPERLINK https:/www.MedChemE/1,3-Dicaffeoylquinic-acid.html acid(1,3-O-Dicaffeoylquinic acid; 1,5-Dicaffeoylquinic acid) Cat. No.: HY-N1412 HYPERLINK https:/www.MedChemE/10-debc-hydrochloride.html 10-DEBC HYPERLINK https:/www.MedChemE/10-debc-hydroch

10、loride.html HYPERLINK https:/www.MedChemE/10-debc-hydrochloride.html hydrochlorideCat. No.: HY-1006541,3-Dicaffeoylquinic acid is a caffeoylquinic acidderivative that exhibits antioxidant activity andradical scavenging activity.10-DEBC hydrochloride is a selective Aktinhibitor, with an IC of 1.28 M.

11、 10-DEBChydrochloride is a novel anti-TB compound.Purity: 98.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/24-methylenecycloartanyl-ferulate.html 24-Methylenecycloartanyl HY

12、PERLINK https:/www.MedChemE/24-methylenecycloartanyl-ferulate.html HYPERLINK https:/www.MedChemE/24-methylenecycloartanyl-ferulate.html ferulate HYPERLINK https:/www.MedChemE/24-methylenecycloartanyl-ferulate.html HYPERLINK https:/www.MedChemE/25-r-s-ruscogenin.html 25(R,S)-RuscogeninCat. No.: HY-N8

13、122 Cat. No.: HY-N513624-Methylenecycloartanyl ferulate is a -oryzanolcompound. 24-Methylenecycloartanyl ferulatepromotes parvin-beta expression in human breastcancer cells. 24-Methylenecycloartanyl ferulate isa potential ATP-competitive Akt1 inhibitor(EC = 33.3M).Purity: 98%Clinical Data: No Develo

14、pment ReportedSize: 5 mg, 10 mg, 25 mgRuscogenin suppresses HCC metastasis by reducingthe expression of MMP-2, MMP-9, uPA, VEGF andHIF-1 via regulating the PI3K/Akt/mTORsignaling pathway. And Ruscogenin alleviatesLPS-induced pulmonary endothelial cell apoptosisby su.Purity: 99.84%Clinical Data: No D

15、evelopment ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/3-4-5-tricaffeoylquinic-acid.html 3,4,5-Tricaffeoylquinic HYPERLINK https:/www.MedChemE/3-4-5-tricaffeoylquinic-acid.html HYPERLINK https:/www.MedChemE/3-4-5-tricaffeoylquinic-acid.html acid HYPERLINK https:/www.MedChe

16、mE/3-4-5-tricaffeoylquinic-acid.html HYPERLINK https:/www.MedChemE/3cai.html 3CAI(3,4,5-triCQA) Cat. No.: HY-N6588Cat. No.: HY-166663,4,5-Tricaffeoylquinic acid (3,4,5-triCQA)inhibits tumor necrosis factor-stimulatedproduction of inflammatory mediators inkeratinocytes via suppression of Akt- andNF-B

17、-pathways.3CAI is a potent and specific AKT1 and AKT2inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/8-aminoadenosine.html 8-Aminoadenosine HYPERL

18、INK https:/www.MedChemE/8-aminoadenosine.html HYPERLINK https:/www.MedChemE/A-443654.html A-443654(8-NH2-Ado) Cat. No.: HY-125927Cat. No.: HY-104258-Aminoadenosine (8-NH2-Ado), a RNA-directednucleoside analogue, reduces cellular ATP levelsand inhibits mRNA synthesis. 8-Aminoadenosineblocks Akt/mTOR

19、signaling and inducesautophagy and apoptosis in a p53-independentmanner. 8-Aminoadenosine has antitumor activity.A-443654 is a pan-Akt inhibitor and has equalpotency against Akt1, Akt2, or Akt3 withincells (K=160 pM).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.04%Clin

20、ical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/a-674563.html A-674563 HYPERLINK https:/www.MedChemE/a-674563.html HYPERLINK https:/www.MedChemE/A-674563-hydrochloride.html A-674563 HYPERLIN

21、K https:/www.MedChemE/A-674563-hydrochloride.html HYPERLINK https:/www.MedChemE/A-674563-hydrochloride.html hydrochlorideCat. No.: HY-13254 Cat. No.: HY-13254AA-674563 is an orally active and selective Akt1inhibitor with a K of 11 nM.A-674563 hydrochloride is a potent and selectiveAkt1 inhibitor wit

22、h K of 11 nM.Purity: 99.87%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/act001.html ACT001 HYPERLINK https:/www.MedChemE/act001.html HYPERLIN

23、K https:/www.MedChemE/actein.html ActeinCat. No.: HY-128861A Cat. No.: HY-N6872ACT001 is an orally active PAI-1 inhibitor byinhibiting the phosphorylation of PI3K and AKT.ACT001 inhibits the phosphorylation of STAT3 andPD-L1 expression by directly binding to STAT3.Actein is a triterpene glycoside is

24、olated from therhizomes of Cimicifuga foetida. Acteinsuppresses cell proliferation, induces autophagyand apoptosis through promoting ROS/JNKactivation, and blunting AKT pathway in humanbladder cancer. Actein has little toxicity in vivo.Purity: 99.62%Clinical Data: No Development ReportedSize: 10 mM

25、1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.58%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/Afuresertib.html Afuresertib(GSK2110183) Cat. No.: HY-15727 HYPERLINK https:/www.MedChemE/Afuresertib-hydrochloride.html Afuresertib HYPERLINK https:/www.MedChemE/Afuresertib-h

26、ydrochloride.html HYPERLINK https:/www.MedChemE/Afuresertib-hydrochloride.html hydrochloride(GSK2110183 hydrochloride) Cat. No.: HY-15727AAfuresertib (GSK2110183) is an orallybioavailable, selective, ATP-competitive andpotent pan-Akt kinase inhibitor with Ks of0.08/2/2.6 nM for Akt1/Akt2/Akt3, respe

27、ctively.Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailable,selective, ATP-competitive and potent pan-Aktkinase inhibitor with Ks of 0.08/2/2.6 nM forAkt1/Akt2/Akt3 respectively.Purity: 99.54%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.02%C

28、linical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AKT-inhibitor-VIII.html AKT HYPERLINK https:/www.MedChemE/AKT-inhibitor-VIII.html HYPERLINK https:/www.MedChemE/AKT-inhibitor-VIII.html inhibitor HYPERLINK https:/www.MedChemE/AKT-inhibitor-VIII.html HYPE

29、RLINK https:/www.MedChemE/AKT-inhibitor-VIII.html VIII HYPERLINK https:/www.MedChemE/AKT-inhibitor-VIII.html HYPERLINK https:/www.MedChemE/AKT-Kinase-Inhibitor.html AKT HYPERLINK https:/www.MedChemE/AKT-Kinase-Inhibitor.html HYPERLINK https:/www.MedChemE/AKT-Kinase-Inhibitor.html Kinase HYPERLINK ht

30、tps:/www.MedChemE/AKT-Kinase-Inhibitor.html HYPERLINK https:/www.MedChemE/AKT-Kinase-Inhibitor.html Inhibitor(AKTi-1/2) Cat. No.: HY-10355Cat. No.: HY-10249AAKT inhibitor VIII (AKTi-1/2) is a cell-permeablequinoxaline compound that has been shown topotently, selectively, allosterically, andreversibl

31、y inhibit Akt1, Akt2, and Akt3activity with IC s of 58 nM, 210 nM, and 2119 nM,respectively.AKT Kinase Inhibitor is an Akt kinase inhibitorwith anti-tumor activity.Purity: 98.93%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 50 mg, 100 mgPurity: 99.56%Clinical Data: No Development Rep

32、ortedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/AKT-IN-1.html AKT-IN-1 HYPERLINK https:/www.MedChemE/AKT-IN-1.html HYPERLINK https:/www.MedChemE/akt-in-10.html AKT-IN-10Cat. No.: HY-18296 Cat. No.: HY-144060AKT-IN-1 is an allosteric AKT inhibitor with anIC of 1.042 M.AKT-IN-10 is a

33、potent inhibitor of AKT. Proteinkinase B (PKB, also known as AKT) is central toPI3K/AKT/mTOR signaling in cells, and its functionis important for cell growth, survival,differentiation and metabolism.Purity: 98.41%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98%Clinical

34、Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/akt-in-11.html AKT-IN-11 HYPERLINK https:/www.MedChemE/akt-in-11.html HYPERLINK https:/www.MedChemE/AKT-IN-2.html AKT-IN-2Cat. No.: HY-144253 Cat. No.: HY-112148AKT-IN-11 is one of the most effectiveantibacteri

35、al agents against human hepatomaBEL-7402 cell line with an IC value of 1.15M.AKT-IN-2 is a potent, selective and orallybioavailable AKT inhibitor with an IC of 5 nMfor AKT1.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

36、 mg HYPERLINK https:/www.MedChemE/akt-in-3.html AKT-IN-3 HYPERLINK https:/www.MedChemE/akt-in-3.html HYPERLINK https:/www.MedChemE/akt-in-5.html AKT-IN-5Cat. No.: HY-126257 Cat. No.: HY-138767AKT-IN-3 (compound E22) is a potent, orally activelow hERG blocking Akt inhibitor, with 1.4 nM, 1.2nM and 1.

37、7 nM for Akt1, Akt2 and Akt3,respectively.AKT-IN-5 (Example 8) is a Akt inhibitor with ICvalues of 450 nM and 400 nM for Akt1 and Akt2,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www

38、.MedChemE/akt-in-6.html AKT-IN-6 HYPERLINK https:/www.MedChemE/akt-in-6.html HYPERLINK https:/www.MedChemE/akt-in-7.html AKT-IN-7Cat. No.: HY-19982 Cat. No.: HY-143610AKT-IN-6 (Example 13) is a potent Akt inhibitor.AKT-IN-6 inhibits Akt1, Akt2 and Akt3 with IC s98%Clinical Data: No Development Repor

39、tedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/akt-in-8.html AKT-IN-8 HYPERLINK https:/www.MedChemE/akt-in-8.html HYPERLINK https:/www.MedChemE/akt-in-9.html AKT-IN-9Cat. No.: HY-143611 Cat. No.: HY-144059AKT-IN-8 is a potent AKT inhibitor with IC s of4.46, 2.44, and 9.47 nM for AKT1, AKT2, and A

40、KT3,respectively.AKT-IN-9 is a potent inhibitor of AKT. Proteinkinase B (PKB, also known as AKT) is central toPI3K/AKT/mTOR signaling in cells, and its functionis important for cell growth, survival,differentiation and metabolism.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurit

41、y: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Akt1-and-Akt2-IN-1.html Akt1 HYPERLINK https:/www.MedChemE/Akt1-and-Akt2-IN-1.html HYPERLINK https:/www.MedChemE/Akt1-and-Akt2-IN-1.html and HYPERLINK https:/www.MedChemE/Akt1-and-Akt2-IN-1.html HYPERLINK http

42、s:/www.MedChemE/Akt1-and-Akt2-IN-1.html Akt2-IN-1 HYPERLINK https:/www.MedChemE/Akt1-and-Akt2-IN-1.html HYPERLINK https:/www.MedChemE/aktide-2t.html AKTide-2TCat. No.: HY-50862 Cat. No.: HY-P1115Akt1 and Akt2-IN-1 is an allosteric inhibitor ofAkt1 (IC =3.5 nM) and (IC =42 nM), withAkt2 potent and ba

43、lanced activity.AKTide-2T is an excellent in vitro substrate forAKT and shows competitive inhibition of histoneH2B phosphorylation with a K of 12 nM. AKTide-2Tmimics the optimal phosphorylation sequence of Aktand is an inhibitory peptide with the wildtypeAKTide lacking Thr in the S22 position.Purity

44、: 99.59%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 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/aktide-2t-tfa.html AKTide-2T HYPERLINK https:/www.MedChe

45、mE/aktide-2t-tfa.html HYPERLINK https:/www.MedChemE/aktide-2t-tfa.html TFA HYPERLINK https:/www.MedChemE/aktide-2t-tfa.html HYPERLINK https:/www.MedChemE/api-1.html API-1Cat. No.: HY-P1115A Cat. No.: HY-110077AKTide-2T TFA is an excellent in vitro substratefor AKT and shows competitive inhibition of

46、histone H2B phosphorylation with a K of 12 nM.API-1, a potent Akt/PKB inhibitor, binds to thePH domain and inhibits Akt membrane translocation.API-1 efficiently reduces the phosphorylationlevels of Akt with an IC of 0.8 M. API-1 isselective for PKB and does not inhibit theactivation of PKC, and PKA.

47、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/apn-akt-in-1.html APN/AKT-IN-1 HYPERLINK https:/www.MedChemE/apn-akt-in-1.html HYPERLINK https:/www.MedChemE/arnicolide-d.html Arnicolide H

48、YPERLINK https:/www.MedChemE/arnicolide-d.html HYPERLINK https:/www.MedChemE/arnicolide-d.html DCat. No.: HY-145244 Cat. No.: HY-N6843APN/AKT-IN-1 is a potent and dual inhibitor of APNand AKT with IC s of 0.21 and 0.27 M,respectively. APN/AKT-IN-1 can effectively inhibitthe phosphorylation of GSK3,

49、the intracellularsubstrate of AKT.Arnicolide D is a sesquiterpene lactone isolatedfrom Centipeda minima. Arnicolide D modulatesthe cell cycle, activates the caspase signalingpathway and inhibits the PI3K/AKT/mTOR andSTAT3 signaling pathways.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg

50、, 5 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/artemisinin.html Artemisinin(Qinghaosu; NSC 369397) Cat. No.: HY-B0094 HYPERLINK https:/www.MedChemE/artemisinin-d4.html Artemisinin-d4(Qinghaosu-d4; NSC 369397-d4) Cat. No.: HY-B0094S1Artemisini

51、n (Qinghaosu), a sesquiterpene lactone,is an anti-malarialdrug isolated from theaerial parts of Artemisia annua L. plants.Artemisinin inhibits AKT signaling pathway bydecreasing pAKT in a dose-dependent manner.Artemisinin-d4 (Qinghaosu-d4) is the deuteriumlabeled Artemisinin. Artemisinin (Qinghaosu)

52、, asesquiterpene lactone, is an anti-malarial drugisolated from the aerial parts of Artemisiaannua L. plants.Purity: 99.03%Clinical Data: LaunchedSize: 10 mM 1 mL, 200 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/at13148.html AT13148 HYPER

53、LINK https:/www.MedChemE/at13148.html HYPERLINK https:/www.MedChemE/AT7867.html AT7867Cat. No.: HY-16071 Cat. No.: HY-12059AT13148 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/II, resp

54、ectively.AT7867 is a potent ATP-competitive inhibitor ofAkt1/Akt2/Akt3 and p70S6K/PKA with IC s of 32nM/17 nM/47 nM and 85 nM/20 nM, respectively.Purity: 99.42%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg

55、, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html AT7867 HYPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html HYPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/AT7867-dihydrochloride.html HYPERLINK https:/www.M

56、edChemE/batatasin-iii.html Batatasin HYPERLINK https:/www.MedChemE/batatasin-iii.html HYPERLINK https:/www.MedChemE/batatasin-iii.html IIICat. No.: HY-12059A Cat. No.: HY-122965AT7867 dihydrochloride is a potent ATP-competitiveinhibitor of Akt1/Akt2/Akt3 and p70S6K/PKAwith IC s of 32 nM/17 nM/47 nM

57、and 85 nM/20 nM,respectively.Batatasin III, a stilbenoid, inhibits cancermigration and invasion by suppressing epithelialto mesenchymal transition (EMT) and FAK-AKTsignals. Batatasin III has anti-cancer activities.Purity: 99.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50

58、mg, 100 mgPurity: 99.70%Clinical Data: No Development ReportedSize: 5 mg, 10 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/BAY1125976.html BAY1125976 HYPERLINK https:/www.MedChemE/BAY1125976.html HYPERLINK https:/www.MedChemE/Borussertib.html BorussertibCat. No.: HY-100018 Cat. No.: HY-122913BAY112

59、5976 is a selective allosteric Akt1/Akt2inhibitor; inhibits Akt1 and Akt2 activity withIC values of 5.2 nM and 18 nM at 10 M ATP,respectively.Borussertib is a covalent-allosteric andfirst-in-class inhibitor of protein kinase Akt,with an IC of 0.8 nM and a of 2.2 nM forKiAkt.Purity: 99.74%Clinical Da

60、ta: Phase 1Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.59%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/AZD5363.html Capivasertib(AZD5363) Cat. No.: HY-15431 HYPERLINK https:/www.MedChemE/cay10404.html CAY10404Cat. No.: HY-1