产品描述: | APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling |
靶点: |
KSR2:120 nM (IC50);MEK1;MEK; MAPK |
体外研究: |
APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells. APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations |
参考文献: |
1. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116. |
溶解性: |
DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.359 ml |
11.795 ml |
23.591 ml |
5 mM |
0.472 ml |
2.359 ml |
4.718 ml |
10 mM |
0.236 ml |
1.18 ml |
2.359 ml |
50 mM |
0.047 ml |
0.236 ml |
0.472 ml |
|
注意: |
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