AG490
Unsuitables - unsuitable to be used as a chemical probe
Structure
This is unsuitable as a chemical probe: While this
compound has been used to interrogate specific protein
targets, it is not a chemical probe and should not be used
in assays that depend on a potent and selective modulator
of the protein.
Unsuitable to be used as a chemical probe
Intended target: JAK2; in JAK2 enzyme assays IC50 value exceeded 125 μM; accordingly cellular experiments assessing the phosphorylation of downstream targets, such as STAT5, AKT, and ERK1/2, at a concentration of 100 μM failed to show significant effect of phosphorylated ERK1/2 or AKT, with only modest effects on STAT5 phosphorylation. In a broader screen involving a panel of 441 lipid and protein kinases at 25 μM concentration, inhibitory activity against four kinases: STK17A, STK17B, PDGFRA, and PDGFRB (>70%) was observed. (DOI: 10.1182/blood.V118.21.4780.4780)