APS-2-79 (hydro<wbr/>chloride)

APS-2-79 (hydrochloride)

CAT N°: 22137
Price:

From 49.00 41.65

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 ?M) 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 ?M.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)-4-quinazolinamine, monohydrochloride
  • Correlated keywords
    • 2002381-25-9 APS2-79 APS279 APS-279 BRAF MAPKK KSR-2 MEK-1 HEK-293H 293-H SKMEL239 SKMEL MEL239 A-375 HCT- 116 A-549
  • Product Overview:
    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 ?M) 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 ?M.

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