SB-590885

SB-590885

CAT N°: 16643
Price:

From €74.00 €62.90

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 5-[2-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
  • Correlated keywords
    • cancer inhibitors signal transduction cell intracellular biochemical BRaf MAP kinase MAPKKK Ras family GTPase MEK1/2 ERK1/2 mutation Val600 melanoma melanocytic nevi SB590885 inhibit block activation anchorage-independent cell proliferation wild type V600E B-RafV600E invasion cerebral ischemia
  • Product Overview:
    B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}

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