Eukaryotic-Initiation-Factor-eIF-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Eukaryotic HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Initiation HYPERLINK https:/www.MedChemE/Targets/Eukar

2、yotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Factor HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html (eIF)Eukaryotic initiati

3、on factors (eIFs) are proteins involved in the initiation phase of eukaryotic translation. These proteins help stabilizethe formation of the functional ribosome around the start codon and also provide regulatory mechanisms in translation initiation.Eukaryotic initiation factor 2B (eIF2B) is a guanin

4、e nucleotide-exchange factor which mediates the exchange of GDP (bound toinitiation factor eIF2) for GTP, thus regenerating the active eIF2.GTP complex that is required for peptide-chain initiation. Theactivity of eIF2B is a key control point for eukaryotic protein synthesis and is altered in respon

5、se to viral infection, hormones,nutrients, growth factors and certain stresses.Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis on cappedmRNAs in the cytoplasm. Eukaryotic initiation factor (elF) 4A functions as a subunit of th

6、e initiation factor complex elF4F, whichmediates the binding of mRNA to the ribosome.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Eukaryotic HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Tar

7、gets/Eukaryotic Initiation Factor (eIF).html Initiation HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Factor HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYP

8、ERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html (eIF) HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Eukaryotic In

9、itiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Activators HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html & HYPERLINK https:/www.MedCh

10、emE/Targets/Eukaryotic Initiation Factor (eIF).html HYPERLINK https:/www.MedChemE/Targets/Eukaryotic Initiation Factor (eIF).html Chemicals HYPERLINK https:/www.MedChemE/r-eif4a3-in-2.html (R)-eIF4A3-IN-2 HYPERLINK https:/www.MedChemE/r-eif4a3-in-2.html HYPERLINK https:/www.MedChemE/z-4egi-1.html (Z

11、)-4EGI-1Cat. No.: HY-43913 Cat. No.: HY-19831A(R)-eIF4A3-IN-2 is a less active enantiomer ofeIF4A3-IN-2. eIF4A3-IN-2 is a highly selective andnoncompetitive eukaryotic initiation factor 4A-3(eIF4A3) inhibitor with an IC of 110 nM.50(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is aninhibitor of eIF4E/eIF

12、4G interaction and oftranslation initiation. (Z)-4EGI-1 effectively bindsto eIF4E with an IC of 43.5 M and a value50 Kdof 8.74 M. (Z)-4EGI-1 has anticancer activity.Purity: 95.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.01%Clinical Data: No Development R

13、eportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 250 mg HYPERLINK https:/www.MedChemE/2bact.html 2BAct HYPERLINK https:/www.MedChemE/2bact.html HYPERLINK https:/www.MedChemE/4E1RCat.html 4E1RCatCat. No.: HY-125021 Cat. No.: HY-144272BAct is a highly selective, and orally activeeIF2B (eukaryotic

14、initiation factor 2B) activatorwith an EC of 33 nM. 2BAct prevents50neurological defects caused by a chronicintegrated stress response. 2BAct is able topenetrate the central nervous system (CNS).4E1RCat is an inhibitor of cap-dependenttranslation, and inhibits eIF4E:eIF4GI interaction,with an IC an

15、of 4 M.50Purity: 98.70%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/4E2RCat.html 4E2RCat HYPERLINK https:/www.MedChemE/4E2RCat.html HYPERLINK https:/www.MedChemE/4

16、EGI-1.html 4EGI-1Cat. No.: HY-100733 Cat. No.: HY-198314E2RCat is an inhibitor of eIF4E-eIF4G interactionwith an IC of 13.5 M.504EGI-1 is an inhibitor of eIF4E/eIF4G interaction,with a K of 25 M against eIF4E binding.dPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 1

17、0 mg, 50 mg, 100 mgPurity: 98.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/atps-tetralithium-salt.html ATPS HYPERLINK https:/www.MedChemE/atps-tetralithium-salt.html HYPERLINK https:/www.MedChemE/atps-tetralithium-salt.htm

18、l tetralithium HYPERLINK https:/www.MedChemE/atps-tetralithium-salt.html HYPERLINK https:/www.MedChemE/atps-tetralithium-salt.html salt HYPERLINK https:/www.MedChemE/atps-tetralithium-salt.html (Adenosine-5-O-3-thiotriphosphate HYPERLINK https:/www.MedChemE/Briciclib.html Briciclib(tetralithium salt

19、); ) Cat. No.: HY-108666 (ON 014185) Cat. No.: HY-16366ATPS (tetralithium salt) is a substrate for thenucleotide hydrolysis and RNA unwinding activitiesof eukaryotic translation initiation factor eIF4A.Briciclib (ON 014185) is a derivative of ON013100, and has the potential in targeting eIF4Efor sol

20、id cancers.Purity: 97.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.65%Clinical Data: Phase 1Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cmld012072.html CMLD012072 HYPERLINK https:/www.MedChemE/cmld012072.html HYPERLINK https:/www.MedChemE/c

21、mld012073.html CMLD012073Cat. No.: HY-129768 Cat. No.: HY-129769CMLD012072 is an amidino-rocaglates and is apotent eukaryotic initiation factor 4A (eIF4A)inhibitor. CMLD012072 can induce RNA clamping ofeIF4A1 and eIF4A2 and possess potent anti-neoplasticactivity.CMLD012073 is an amidino-rocaglates a

22、nd is apotent eukaryotic initiation factor 4A (eIF4A)inhibitor. CMLD012073 inhibits the growth ofNIH/3T3 cells with an IC of 10 nM. CMLD01207350inhibits eukaryotic translation initiation bymodifying the behavior of the RNA helicase (eIF4A).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg,

23、 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/cmld012612.html CMLD012612 HYPERLINK https:/www.MedChemE/cmld012612.html HYPERLINK https:/www.MedChemE/cr-1-31-b.html CR-1-31-BCat. No.: HY-1

24、29767 Cat. No.: HY-136453CMLD012612 is an amidino-rocaglate containing ahydroxamate group and is a potent eukaryoticinitiation factor 4A (eIF4A) inhibitor. CMLD012612inhibits cell translation and is cytotoxic toNIH/3T3 cells with an IC value of 2 nM.50CR-1-31-B is a synthetic rocaglate and a potente

25、IF4A inhibitor. CR-1-31-B exhibits powerfulinhibitory effects over eIF4A by perturbing theinteraction between eIF4A and RNA, sequentiallyimpeding initiation during protein synthesis.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.23%Clinical Data: No Development Re

26、portedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/didesmethylrocaglamide.html Didesmethylrocaglamide HYPERLINK https:/www.MedChemE/didesmethylrocaglamide.html HYPERLINK https:/www.MedChemE/eif4a3-in-1.html eIF4A3-IN-1Cat. No.: HY-19356A Cat. No.: HY-101513Didesmethylrocaglamide, a derivat

27、ive ofRocaglamide, is a potent eukaryotic initiationfactor 4A (eIF4A) inhibitor. Didesmethylrocaglamidehas potent growth-inhibitory activity with an IC50of 5 nM.eIF4A3-IN-1 (compound 53a) is a selectiveeukaryotic initiation factor 4A3 (eIF4A3) inhibitor(IC =0.26 M; =0.043 M), which binds to a50 Kdno

28、n-ATP binding site of eIF4A3 and showssignificant cellular nonsense-mediated RNA decay(NMD) inhibition at 10 and 3 M and can be asPurity: 98.40%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 m

29、g, 100 mg HYPERLINK https:/www.MedChemE/eIF4A3-IN-2.html eIF4A3-IN-2 HYPERLINK https:/www.MedChemE/eIF4A3-IN-2.html HYPERLINK https:/www.MedChemE/eif4a3-in-4.html eIF4A3-IN-4Cat. No.: HY-101785 Cat. No.: HY-139872eIF4A3-IN-2 is a highly selective andnoncompetitive eukaryotic initiation factor 4A-3(e

30、IF4A3) inhibitor with an IC of 110 nM.50eIF4A3-IN-4 is a novel eIF4A inhibitor with an IC50value of 8.6 M.Purity: 99.77%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/ei

31、f4a3-in-5.html eIF4A3-IN-5 HYPERLINK https:/www.MedChemE/eif4a3-in-5.html HYPERLINK https:/www.MedChemE/eif4a3-in-6.html eIF4A3-IN-6Cat. No.: HY-145359 Cat. No.: HY-145360eIF4A3-IN-5 is a potent inhibitor of eukaryoticinitiation factor 4A (eIF4A), such as eIF4AI andeIF4AII. eIF4A3-IN-5 has the poten

32、tial for theresearch of eIF4A dependent diseases, including theresearch of cancer (extracted from patentUS20170145026A1).eIF4A3-IN-6 is a potent inhibitor of eukaryoticinitiation factor 4A (eIF4A), such as eIF4AI andeIF4AII. eIF4A3-IN-6 has the potential for theresearch of eIF4A dependent diseases,

33、including theresearch of cancer (extracted from patentUS20170145026A1).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/eif4a3-in-7.html eIF4A3-IN-7 HYPERLINK https:/www.MedChemE/eif4a3-in

34、-7.html HYPERLINK https:/www.MedChemE/eif4e-in-1.html eIF4E-IN-1Cat. No.: HY-145361 Cat. No.: HY-145240eIF4A3-IN-7 is a potent inhibitor of eIF4A3.eIF4A3-IN-7 has the potential for researchingcancer and other dysproliferative diseases(extracted from patent WO2019161345A1, Compound8).eIF4E-IN-1 is a

35、potent inhibitor of eIF4E.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/eif4e-in-2.html eIF4E-IN-2 HYPERLINK https:/www.MedChemE/eif4e-in-2.html HYPERLINK https:/www.MedCh

36、emE/eif4e-in-3.html eIF4E-IN-3Cat. No.: HY-145262 Cat. No.: HY-145309eIF4E-IN-2 is a potent inhibitor of eukaryoticinitiation factor 4e (eIF4e). eIF4E-IN-2 has thepotential for researching eIF4e dependent diseases,including the research of cancer (extracted frompatent WO2021003157A1, compound 1188).

37、eIF4E-IN-3 is a potent inhibitor of eukaryoticinitiation factor 4e (eIF4e). eIF4E-IN-3 has thepotential for researching eIF4e dependent diseases,including the research of cancer (extracted frompatent WO2021003157A1, compound 485).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurit

38、y: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Episilvestrol.html EpisilvestrolCat. No.: HY-15359 HYPERLINK https:/www.MedChemE/GCN2-IN-1.html GCN2-IN-1(A-92) Cat. No.: HY-100877Episilvestrol is a derivative of silvestrol,isolated from the fruits and twigs

39、 of Aglaiasilvestris, and is a specific eIF4A-targetingtranslation inhibitor, with antitumor activity.GCN2-IN-1 (A-92) is a potent general controlnonderepressible 2 kinase (GCN2) inhibitor withan IC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Rocaglamide.html Rocaglamide HYPERLINK https:/www.MedChemE/Rocaglamide.html HYPERLINK https:/www.MedChemE/SBI-0640756.html SBI-0640756(Roc-A) Cat. No.: HY-19356 (SBI-