IC50 values of the p110 isoform-specific PI3K inhibitors with pure p110 enzymes
Inhibitor . | Abbreviation . | IC50, μM . | |||
---|---|---|---|---|---|
p110α . | p110β . | p110γ . | p110δ . | ||
PIK-90 | 1 | 0.011 | 0.35 | 0.018 | 0.058 |
PIK-93 | 2 | 0.039 | 0.59 | 0.016 | 0.12 |
PI-103 | 3 | 0.008 | 0.088 | 0.015 | 0.048 |
TGX-221 | 4 | 5.0 | 0.005 | > 10.0 | 0.1 |
SW18 | 5 | 6.7 | 2.4 | 0.038 | 0.005 |
SW30 | 6 | 85 | 0.74 | 1.3 | 0.007 |
AS605240 | 7 | 0.06 | 0.27 | 0.008 | 0.3 |
Inhibitor . | Abbreviation . | IC50, μM . | |||
---|---|---|---|---|---|
p110α . | p110β . | p110γ . | p110δ . | ||
PIK-90 | 1 | 0.011 | 0.35 | 0.018 | 0.058 |
PIK-93 | 2 | 0.039 | 0.59 | 0.016 | 0.12 |
PI-103 | 3 | 0.008 | 0.088 | 0.015 | 0.048 |
TGX-221 | 4 | 5.0 | 0.005 | > 10.0 | 0.1 |
SW18 | 5 | 6.7 | 2.4 | 0.038 | 0.005 |
SW30 | 6 | 85 | 0.74 | 1.3 | 0.007 |
AS605240 | 7 | 0.06 | 0.27 | 0.008 | 0.3 |
The IC50 values using intact cells are 10 to 100 times higher.30