1,3-DIHYDRO-1-(1-((4-(6-PHENYL-1H-IMIDAZO[4,5-G]QUINOXALIN-7-YL)PHENYL)METHYL)-4-PIPERIDINYL)-2H-BENZIMIDAZOL-2-ONE TRIFLUOROACETATE SALT HYDRATE Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
Akt plays a role in signal transduction pathways of cell proliferation, apoptosis, angiogenesis, and diabetes. Akt1 and Akt2 dual kinase inhibitors are capable of sensitizing tumor cells to certain apoptotic stimuli, and inhibit Akt phosphorylation
in vivo. Akt1 kinase activity and its regulation by extracellular signaling factors
in vivo in hematopoietic cells suggests the activation of AKT1 involves intracellular translocation of the kinase from cytosol to membrane.
Biochem/physiol Actions
Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.
1,3-DIHYDRO-1-(1-((4-(6-PHENYL-1H-IMIDAZO[4,5-G]QUINOXALIN-7-YL)PHENYL)METHYL)-4-PIPERIDINYL)-2H-BENZIMIDAZOL-2-ONE TRIFLUOROACETATE SALT HYDRATE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
