Table 3.
Inhibitors of cardiomyocyte hypertrophy: kinase inhibitor hits.
| Compound | % Inhibition PE
|
% Inhibition PMA
|
Target | ||
|---|---|---|---|---|---|
| Cell area | ANF | Cell area | ANF | ||
| AZD8055 | >100 | >100 | >100 | >100 | mTOR |
| WYE-125132 | >100 | >100 | >100 | >100 | mTOR |
| GDC-0980 | >100 | 84 | >100 | 84 | mTOR/PI3K |
| PF-04691502 | >100 | 75 | >100 | 97 | mTOR/PI3K |
| BEZ235 | >100 | 88 | >100 | >100 | mTOR/PI3K |
| Pelitinib | >100 | >100 | >100 | >100 | EGFR |
| WZ3146 | >100 | >100 | >100 | >100 | EGFR |
| WZ4002 | >100 | >100 | >100 | >100 | EGFR |
| AEE788 | 97 | 82 | 82 | 79 | EGFR/Her1-2/VEGFR |
| OSI-930 | >100 | >100 | >100 | 85 | c-Kit/VEGFR |
| Hesperadin | >100 | >100 | 82 | >100 | Aurora |
| Aurora A Inhibitor I | >100 | >100 | >100 | >100 | Aurora |
| ENMD-2076 | 81 | 79 | 92 | 76 | Aurora/Flt-3/Src |
| TG101209 | >100 | 100 | >100 | 98 | FLT-3/JAK |
| NVP-BSK805 | >100 | 79 | >100 | 93 | JAK |
| PHA-793887 | >100 | >100 | >100 | >100 | CDK |
| AZD7762 | >100 | >100 | 71 | 96 | CHK |
| Crizotinib | >100 | >100 | >100 | >100 | c-Met/ALK |
| BI 2536 | >100 | >100 | >100 | >100 | PLK |
| Bosutinib | >100 | >100 | >100 | >100 | Src |
| Vinorelbinea | >100 | −11 | >100 | 24 | P38 MAPK |
| ON-01910a | >100 | −1 | 88 | −28 | PLK |
| KX2-391a | >100 | −60 | 74 | −39 | Src |
Kinase inhibitors were screened at 1 mu;M.
a
Class II hits (no inhibition of ANF expression).