Specificity profiles of the PI3K inhibitors used in this study, based on IC50 values (μM)
Name . | p110α . | p110β . | p110γ . | p110δ . | Comment . |
---|---|---|---|---|---|
Ly294002 | 9.3 | 2.9 | 38 | 6.0 | Pan-PI3K inhibitor |
PIK-90 | 0.011 | 0.35 | 0.018 | 0.058 | Low mTOR activity, cell permeable |
PI-103 | 0.008 | 0.088 | 0.15 | 0.048 | Targets PI3KC2β, mTORC2, DNA-PK, p235 |
TGX115 | 61 | 0.13 | 100 | 0.63 | p110β- and δ-selective |
IC87114 | 200 | 16 | 61 | 0.13 | Selective p110δ inhibitor, cell permeable |
Name . | p110α . | p110β . | p110γ . | p110δ . | Comment . |
---|---|---|---|---|---|
Ly294002 | 9.3 | 2.9 | 38 | 6.0 | Pan-PI3K inhibitor |
PIK-90 | 0.011 | 0.35 | 0.018 | 0.058 | Low mTOR activity, cell permeable |
PI-103 | 0.008 | 0.088 | 0.15 | 0.048 | Targets PI3KC2β, mTORC2, DNA-PK, p235 |
TGX115 | 61 | 0.13 | 100 | 0.63 | p110β- and δ-selective |
IC87114 | 200 | 16 | 61 | 0.13 | Selective p110δ inhibitor, cell permeable |
The IC50 values and the key characteristics of the inhibitors are based on the data published by Knight et al53 and Marone et al.35