Isozyme selective Akt1/2 kinase inhibitor. The Akt1/2 kinase inhibitor shows in in vitro kinase assays inhibiton of IC50 = 58 nM for Akt1 and respectively 210 nM, and 2.12 mM for Akt2, and Akt3. The observed selectivity has been attributed to an allosteric mode of binding, noncompetitive with ATP, wherein Akt inhibition is dependent on the presence of the pleckstrin homology (PH) domain. Importantly, these Akt inhibitors has no inhibitory effect against closely related AGC family (PKA, PKC, SGK) even at concentrations as high as 50 μM. Formula: C34H29N7O · xC2HF3O2 · yH2O, Molecular Weight:  551.64 g/mol (free base basis), Appearance:  solid, Purity:  >98%, Solubility: soluble in DMSO: 12 mg/mL

Product specific literature references:

Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE, Duggan ME, Lindsley CW. (2005) „Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors." Bioorg Med Chem Lett. 15(4) 905-909

Barnett SF, Defeo-Jones D, Fu S, Hancock PJ, Haskell KM, Jones RE, Kahana JA, Kral AM, Leander K, Lee LL, Malinowski J, McAvoy EM, Nahas DD, Robinson RG, Huber HE. "Identification and characterization of pleckstrin-homology-domain-dependent and isoen-zyme-specific Akt inhibitors." Biochem. J. 385, 399-408, (2005)

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This product was added to our catalog on May 11, 2007


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