Table 1.

PKA inhibitors tested

DrugKi PKAKi against other kinasesEC50 FLCEC50 PHH
H8948 nmol/LPKG 480 nmol/LFLC1 5.82 μmol/L41.5 μmol/L
FLC2 23.88 μmol/L
FLC3 18.17 μmol/L
FLC4 20.94 μmol/L
FLC5 9.49 μmol/L
KT572060 nmol/LPKG/PKC >2 μmol/LFLC1 1.61 μmol/L>10 μmol/L
FLC2 2.14 μmol/L
FLC3 2.71 μmol/L
FLC4 1.48 μmol/L
FLC5 3.87 μmol/L
A-67456316 nmol/LAkt1 11 nmol/LFLC1 0.34 μmol/L3.45 μmol/L
CDK2 46 nmol/LFLC2 0.7 μmol/L
GSK-3β 110 nmol/LFLC3 0.88 μmol/L
ERK2 260 nmol/LFLC4 0.16 μmol/L
PKCδ 360 nmol/LFLC5 3.45 μmol/L
RSK2 580 nmol/L
Capivasertib (AZD5363)7 nmol/LAkt1 3 nmol/LFLC1 2.98 μmol/L>10 μmol/L
Akt2 8 nmol/LFLC2 3.85 μmol/L
Akt3 8 nmol/LFLC3 5.15 μmol/L
FLC4 2.09 μmol/L
FLC5 12.6 μmol/L
AT131483 nmol/LAkt1 38 nmol/LFLC1 0.039 μmol/L4.05 μmol/L
Akt2 402 nmol/LFLC2 6.14 μmol/L
Akt3 50 nmol/LFLC3 0.59 μmol/L
p70s6k 8 nmol/LFLC4 4.29 μmol/L
Rock1 6 nmol/LFLC5 0.096 μmol/L
Rock2 4 nmol/L
Uprosertib (GSK2141795)2 nmol/LAkt1 180 nmol/LFLC1 0.049 μmol/L>10 μmol/L
Akt2 328 nmol/LFLC2 5.039 μmol/L
Akt3 38 nmol/LFLC3 0.87 μmol/L
FLC4 0.91 μmol/L
FLC5 1.72 μmol/L