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| | in vitro Kinase Assay |
| Description: | Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human enzymes: the BMP type-I receptor activin receptor-like kinase 2 (ALK2/BMPR-I), the TGFβ type-I receptor activin receptor-like kinase 5 (ALK5/ TGFβR-I), the VEGF type-2 receptor (VEGFR2/KDR), the AMP-activated protein kinase (AMPK), and the platelet-derived growth factor receptor-β (PDGFR β). In in vitro kinase assays, DM was relatively nonspecific, targeting ALK2, AMPK, and KDR with IC50s of <250 nM. LDN-193189 was slightly more selective but still had significant effects against ALK5 and KDR. By comparison, DMH1, DMH2, and DMH3 were much more selective ALK2 inhibitors. In particular, DMH1 had no detectible activity against any of the kinases tested besides ALK2. DMH4 was a selective KDR inhibitor with modest effect on ALK2 (IC50 3.6 uM) and minimal effect on AMPK (IC50 8.0 uM). Nonspecific kinase inhibitor staurosporine was used as a control. All of the reactions were carried out in the presence of 10 uM ATP. |
| Affinity data for this assay | |
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