Table 1.

Selectivity of Akt inhibitors for selected kinases

FamilyKinaseA-443654 fold (Ki, μmol/L)A-674563 fold (Ki, μmol/L)
AGCAkt11 (0.00016)1 (0.011)
PKA40 (0.0063)1.4 (0.016)
PKCγ150 (0.024)110 (1.2)
PKCδ200 (0.033)32 (0.36)
PDK1>120,000 (>20)>1,800 (>20)
TKKDR19,000 (3.1)>330 (>3.7)
cKIT7,300 (1.2)>530 (>5.8)
SRC16,000 (2.6)1,200 (13)
Flt122,000 (3.6)>200 (>2.2)
CMGCCDK2150 (0.024)4.2 (0.046)
ERK22,100 (0.34)24 (0.26)
GSK3β260 (0.041)10 (0.11)
CK215,000 (2.4)490 (5.4)
CAMKChk115,000 (2.3)235 (2.6)
RSK268 (0.011)53 (0.58)
MAPK-AP221,000 (3.3)100 (1.1)
  • NOTE: The fold selectivity versus Akt1 is shown for each kinase and the Ki is in parentheses.

    Abbreviations: PDK1, phosphatidylinositide-dependent kinase 1; MAPK, mitogen-activated protein kinase; GSK3, glycogen synthase kinase 3; ERK2, extracellular signal–regulated kinase 2.