Table 2. Sequence and activity of variegin and its variants.
Name | Sequence | Pre-incubation tine (min) | IC50 (nM) | Ki (nM) | Mechanism | Plots shown in figure |
s-variegin | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 8.25±0.45 | 0.318±0.020 | Fast, tight-binding, competitive | Published [17] |
20 | 10.4±0.3 | |||||
EP25 | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 173±26 | 0.365±0.109 | Slow, tight-binding, competitive | S3 |
20 | 13.1±0.7 | |||||
MH22 | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 11.5±0.7 | 14.1±0.3 | Fast, tight-binding, noncompetitive | Published [17] |
20 | 12.3±1.9 | |||||
Hirulog-1 | D FPRPGGGGNGDFEEIPEEYL | 0 | 72.6±3.9 | 2.94±0.12 | Fast, tight-binding, competitive | Published [17] |
10 | 102±13 | |||||
EP21 | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 177±7 | 0.315±0.024 | Slow, tight-binding, competitive | S4 |
20 | 16.2±2.9 | |||||
MH18 | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 10.9±1.2 | 14.9±3.5 | Fast, tight-binding, noncompetitive | S5 |
20 | 11.7±1.9 | |||||
DV24 | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 7.49±0.28 | 0.306±0.029 | Fast, tight-binding, competitive | S7 |
20 | 10.1±0.6 | |||||
DV24H12A | SDQGDVAEPKMAKTAPPFDFEAIPEEYLDDES | 0 | 48.2±12.4 | 3.23±0.48 | Fast, tight-binding, competitive | S8 |
20 | 141±11 | |||||
MH18H12A | SDQGDVAEPKMAKTAPPFDFEAIPEEYLDDES | 0 | 328±23 | 329±8 | Fast, tight-binding, noncompetitive | S9 |
20 | 343±46 | |||||
DV24K10R | SDQGDVAEPRMHKTAPPFDFEAIPEEYLDDES | 0 | 6.98±0.76 | 0.259±0.015 | Fast, tight-binding, competitive | S10 |
20 | 12.0±0.4 | |||||
DV23 | SDQGDVAEPKMHKTAPPFDFEAIPEEYLDDES | 0 | 45.4±1.6 | 2.19±0.23 | Fast, tight-binding, competitive | S11 |
20 | 77.8±6.1 | |||||
DV23K10R | SDQGDVAEPRMHKTAPPFDFEAIPEEYLDDES | 0 | 12.9±1.0 | 0.600±0.010 | Fast, tight-binding, competitive | S12 |
20 | 102±1 | |||||
EP25A22E | SDQGDVAEPKMHKTAPPFDFEEIPEEYLDDES | 0 | 124±23 | 0.311±0.070 | Slow, tight-binding, competitive | S13 |
20 | 13.5±2.1 | |||||
MH22A22E | SDQGDVAEPKMHKTAPPFDFEEIPEEYLDDES | 0 | 13.6±0.5 | 15.1±1.0 | Fast, tight-binding, noncompetitive | S14 |
20 | 15.6±0.4 | |||||
DV24Yphos | SDQGDVAEPKMHKTAPPFDFEAIPEEY¶LDDE | 0 | 8.67±0.45 | 0.327±0.032 | Fast, tight-binding, competitive | S15 |
20 | 12.4±1.2 | |||||
DV24K10RYphos | SDQGDVAEPRMHKTAPPFDFEAIPEEY¶LDDES | 0 | 4.64±0.78 | 0.150±0.018 | Fast, tight-binding, competitive | S16 |
20 | 7.80±1.80 | |||||
DV24Ysulf | SDQGDVAEPKMHKTAPPFDFEAIPEEY*LDDE | 0 | 1.66±0.18 | 0.0560±0.0180 | Fast, tight-binding, competitive | S17 |
20 | 2.02±0.29 | |||||
DV24K10RYsulf | SDQGDVAEPRMHKTAPPFDFEAIPEEY*LDDE | 0 | 1.39±0.17 | 0.0420±0.0061 | Fast, tight-binding, competitive | S18 |
20 | 1.66±0.21 | |||||
MH18Ysulf | SDQGDVAEPKMHKTAPPFDFEAIPEEY*LDDES | 0 | 1.26±0.18 | 1.25±0.18 | Fast, tight-binding, noncompetitive | S19 |
20 | 1.17±0.14 |
Y¶: phosphotyrosine; Y*: sulfotyrosine.