ERK + 5uM GSK1120212 ERK + 5uM SCH772984 Supplementary Figure S1 TdF binding assay for SCH772984, Vertex 11e and GSK1120212 Tm = -0.15 ± 0.20 K N Bi di Tm = 10.3 ± 0.30 K 0 24 ± 0 14 M K D = No Binding Protein + 5uM Compound Protein only K D = 0.24 ± 0.14 nM Protein + 5uM Compound Protein only ERK + 5uM Vertex 11e MEK + 5uM GSK1120212 ERK + 5uM Vertex 11e Tm =68 ± 13 MEK + 5uM GSK1120212 Tm =80 ± 0 51 Tm = 6.8 ± 1.3 K D = 5.4 ± 2.2 nM Protein + 5uM Compound Protein only Tm = 8.0 ± 0.51 K D = 7.1 ± 2.7 nM Protein + 5uM Compound Protein only MEK + 5uM SCH772984 MEK + 5uM Vertex 11e Tm = -0.17 ± 0.14 K D = No Binding Protein + 5uM Compound Protein only Tm = -0.11 ± 0.13 K D = No Binding Protein + 5uM Compound Protein only
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Supplementary Figure S1 - Cancer Discovery · Supplementary Figure S2 Inhibition of BRAF inhibitor-induced phosphorylation of ERK by SCH772984 in HCT-116 colorectal and Calu-6 non-small
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ERK + 5uM GSK1120212 ERK + 5uM SCH772984
Supplementary Figure S1TdF binding assay for SCH772984, Vertex 11e and GSK1120212
Tm = -0.15 ± 0.20 K N Bi di
Tm = 10.3 ± 0.30K 0 24 ± 0 14 MKD = No Binding
Protein + 5uM CompoundProtein only
KD = 0.24 ± 0.14 nM
Protein + 5uM CompoundProtein only
ERK + 5uM Vertex 11e MEK + 5uM GSK1120212ERK + 5uM Vertex 11e
Supplementary Figure S2Inhibition of BRAF inhibitor-induced phosphorylation of ERK by SCH772984 in HCT-116 colorectal and Calu-6 non-small cell lung cancer lines
PLX4720772984
10uM 1uM 10uM 1uM
+- --- + +
- 10uM
Calu-61uM 10uM 1uM
+- --- + +
-
HCT-116PLX4720
772984
10uM 1uM 10uM 1uM
+- --- + +
- 10uM
Calu-61uM 10uM 1uM
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HCT-116PLX4720
772984
10uM 1uM 10uM 1uM
+- --- + +
- 10uM
Calu-61uM 10uM 1uM
+- --- + +
-
HCT-1161uM 10uM 1uM
+- --- + +
-
HCT-116
772984 + + +300nM
+ + +
pERK
tERK
pMEK
772984 + + +300nM
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pERK
tERK
pMEK
772984 + + +300nM
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pERK
tERK
pMEK
tMEK
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tMEK
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tMEKtMEK
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Supplementary Figure S3Time course of pRSK & pERK suppression in A375 cells treated withSCH772984 or control (DMSO)