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APS-2-79 is a stabilizer of the Kinase suppressor of Ras (KSR) inactive state, resulting in inhibition of oncogenic Ras signaling, antagonizing the Ras–MAPK pathway. KSR is a MAPK scaffold that is regulated allosterically by dimerization with RAF. APS-2-79 was found to bind to the KSR active site with an IC50 value of 120 nM, antagonizing MEK (MAPKK) phosphorylation by RAF. In Ras mutant cell lines, APS-2-79 increased the potency of several MEK inhibitors..
| Molecular Weight | 423.89 |
| Formula | C23H21N3O3 · HCl |
| CAS Number | 2002381-31-7 |
| Solubility (25°C) | DMSO: 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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