TABLE 1.
Kinase profiling data for PV1019
Experiments were performed by Reaction Biology Corp. (http://www.reactionbiology.com/) using a radioactive assay method. Ten concentration curves were run with 10 μM ATP. Kinases showing some inhibition are in bold, and evolutionarily related kinases (Manning et al., 2002) are in italic.
| Kinase | PV1019 IC50 | Kinase | PV1019 IC50 |
|---|---|---|---|
| nM | nM | ||
| ABL1 | >20,000 | IR | >20,000 |
| ALK | >20,000 | IRAK4 | >20,000 |
| AKT1 (dPH, S473D) | 10,900 | JAK2 | >20,000 |
| Aurora A | >20,000 | JAK3 | >20,000 |
| BTK | >20,000 | KDR/VEGFR2 | >20,000 |
| CAMKIIb | >20,000 | LCK | >20,000 |
| CDK1/cyclinB | 1,835 | Lyn | >20,000 |
| CDK2/cyclinA | >20,000 | MINK | 2,261 |
| Chk1 | 15,730 | MST2/STK3 | >20,000 |
| Chk2 | 24 | P38α/MAPK14 | >20,000 |
| c-MET | >20,000 | PAK2 | 8,579 |
| c-Src | >20,000 | PDGFRa | >20,000 |
| DAPK1 | 8,743 | PHKg2 | 5,707 |
| EGFR | >20,000 | PIM1 | 4,749 |
| EphA3 | >20,000 | PKA | 9,469 |
| EphB4 | >20,000 | PKCα | >20,000 |
| ErbB4/HER4 | >20,000 | PLK2 | >20,000 |
| ERK1 | >20,000 | RET | >20,000 |
| ERK2/MAPK2/P42MAPK | >20,000 | ROCK-I | 9,405 |
| FGFR1 | >20,000 | RSK1 | 10,970 |
| FGFR2 | >20,000 | RSK2 | 3,613 |
| FGFR3 | >20,000 | Syk | >20,000 |
| FLT1/VEGFR1 | >20,000 | TAK1-TAB1 | >20,000 |
| FLT3 | >20,000 | TIE2 | >20,000 |
| FLT4 | >20,000 | TRKA/NTRK1 | >20,000 |
| GSK3β | >20,000 | ZAP70 | >20,000 |
| HIPK1 | 10,780 |
ALK, anaplastic lymphoma kinase; BTK, Bruton's tyrosine kinase; CAMK, Ca2+/calmodulin-dependent protein kinase; CDK, cyclin-dependent kinase; CHK, C-terminal Src kinase-homologous kinase; DAPK, death-associated protein kinase; EGFR, epidermal growth factor receptor; Eph, ephrin type A receptor; ERK, extracellular signal-regulated kinase; MAPK, mitogen-activated protein kinase; FGFR, fibroblast growth factor receptor; VEGFR, vascular endothelial growth factor receptor; FLT, FMS-like tyrosine kinase; GSK, glycogen synthase kinase; HIPK, homeodomain interacting protein kinase; IRAK, interleukin-1 receptor-associated kinase; JAK, Janus tyrosine kinase; KDR, kinase insert domain receptor; LCK, lymphocyte-specific protein tryosine kinase; MINK, Misshapen/NIKs-related kinase; MST, mammalian STE20-like kinase; STK, serine/threonine kinase 3; PAK, p21-activated kinase; PDGFR, platelet-derived growth factor receptor; PHKg2, phosphorylase kinase γ2 ; PK, protein kinase; PLK, polo-like kinase; ROCK, Rho-associated kinase; RSK, ribosomal S6 kinase; Syk, spleen tyrosine kinase; TAK, transforming growth factor-β -activated kinase; TAB, transforming growth factor-β-activated protein kinase-binding protein; NTRK, neurotrophic tyrosine kinase receptor; ZAP70, ζ -chain-associated protein kinase 70.