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Beschreibung

A cell permeable pyridoindole based compound that acts as a highly potent and selective inhibitor of breast tumor kinase (Brk, IC50 = 3.15 nM) with minimal or no effect against a panel of more than 30 other protein kinases (IC50 = <10 µ,M for PIM2, NEK1 and2, CAMK4, MAPKAPK3 and 5 and MARK1, 3, and 5). Does not affect the activity of Akt isoforms, AGC kinases, ERK1 and 2, JNK 1 and 2 and HIPK isoforms. Displays anti-proliferative activity against multiple breast cancer cell lines (GI50 = 990 nM, 1.02 µ,M, and 1.58 µ,M for MCF7, HS-578/T, BT-549, respectively).Please note that the molecular weight for this compound is batch-specific due to variable water content., A cell permeable pyridoindole based compound that acts as a highly potent and selective inhibitor of breast tumor kinase (Brk, IC50 = 3.15 nM) with minimal or no effect against a panel of more than 30 other protein kinases (IC50 = <10 µ,M for PIM2, NEK1 and2, CAMK4, MAPKAPK3 and 5 and MARK1, 3, and 5). Does not affect the activity of Akt isoforms, AGC kinases, ERK1 and 2, JNK 1 and 2 and HIPK isoforms. Displays anti-proliferative activity against multiple breast cancer cell lines (GI50 = 990 nM, 1.02 µ,M, and 1.58 µ,M for MCF7, HS-578/T, BT-549, respectively).