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. 2015 Sep 30;5:14538. doi: 10.1038/srep14538

Figure 6. Allosteric ruxolitinib resistant variants activate the enzymatic activity.

Figure 6

(a) A coomassie blue stained gel showing partially purified full length JAK2 and its variants. (b) Steady state enzyme kinetics showing the activation of ruxolitinib resistant mutants except L983F. Variant R683T is highly active, while Y931C showed increased Vmax and and reduced Km(ATP). The Apparent values for Km(ATP) and Vmax are shown on the right side of the graph for each mutant. (c) Dose response analysis against ruxolitinib showing resistance to inhibition. IC50 values for each mutant (as an indirect measure for drug affinity) are indicated on the right side of the graph.