Table 2.
Mutation | Region | IC50mutant/IC50WT* |
---|---|---|
WT | KIR | 1.0 +/− 0.3 |
SOCS1-3 | 0.1 +/− 0.05 | |
L22F | 0.1 +/− 0.03 | |
L22A | 1.2 +/− 0.2 | |
K23A | 1.4 +/− 0.1 | |
T24A | 3.3 +/− 0.5 | |
F25A | no inhibition | |
S26A | 1.0 +/− 0.04 | |
S27A | 2.5 +/− 0.2 | |
K28A | 2.8 +/− 0.7 | |
S29A | ESS | 2.0 +/− 0.3 |
E30A | 23.0 +/− 2.9 | |
Y31A | 6.0 +/− 0.1 | |
Y47F | βA | 80 +/− 20 |
A50E | 1.1 +/− 0.2 | |
A50K | 6.0 +/− 2.0 | |
T52A | 10 +/− 2.0 | |
R77A | BC loop | 1.4 +/− 0.2 |
F79A | no inhibition | |
F80A | no inhibition |
Errors are SD from three independent experiments.
SOCS1-3 refers to a SOCS1/SOCS3 chimera which binds to JAK2 with 5–10 fold higher affinity30