An inhibitor of KSR-dependent MAPK signaling; inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes (IC50 = 120 nM); stabilizes KSR2 in an inactive state; reduces interactions between B-RAF and KSR2-MEK1 complexes; inhibits KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells at 5 μM; enhances the efficacy of trametinib

APS-2-79 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
2002381-31-7
Storage:
-20
UN-No:
Non-Hazardous - /

APS-2-79 is an inhibitor of MAPK signaling dependent on kinase suppressor of Ras (KSR).{45098} It inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes (IC50 = 120 nM), stabilizes KSR2 in an inactive state, and reduces interactions between B-RAF and KSR2-MEK1 complexes.{45098,45099} APS-2-79 (5 μM) inhibits KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells.{45098} It enhances the efficacy of the MEK inhibitor trametinib (Item No. 16292), further reducing cell viability in HCT116 and A549 cell lines containing K-Ras mutations, but not B-RAF mutant SK-MEL-239 and A375 cell lines, when used at a concentration of 1 μM.  

 

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Description

An inhibitor of KSR-dependent MAPK signaling; inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes (IC50 = 120 nM); stabilizes KSR2 in an inactive state; reduces interactions between B-RAF and KSR2-MEK1 complexes; inhibits KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells at 5 μM; enhances the efficacy of trametinib, further reducing cell viability in K-Ras mutant HCT116 and A549 cell lines, but not B-RAF mutant SK-MEL-239 and A375 cell lines, at 1 μM

Formal name: 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)-4-quinazolinamine, monohydrochloride

Synonyms: 

Molecular weight: 423.9

CAS: 2002381-31-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|GTPases

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