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Description

A cell-permeable L-homo-Trp conjugate of lithocholic acid that acts as an Eph receptor antagonist and competitively disrupts Eph2A-ephrin-A1 binding (IC50 = 945 nM, KI = 345 nM). Blocks the interaction of ephrin-A1 and ephrin-B1 with all Eph receptors (IC50 = 840 nM - 1.54 µ,M for EphA and 2.6 - 3.74 µ,M for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µ,M), however, it does not affect tyrosine kinase activity of EGF and VEGF receptors. Slightly reduces PC3 cell proliferation without affecting cell cycle or apoptosis. However, it blocks the rounding effect of ephrin-A1-Fc in PC3 cells (IC50 = 6.25 µ,M). Also shown to inhibit angiogenesis in HUVEC (IC50 = 5.2 µ,M) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µ,M, respectively)., A cell-permeable L-homo-Trp conjugate of lithocholic acid that acts as an Eph receptor antagonist and competitively disrupts Eph2A-ephrin-A1 binding (IC50 = 945 nM, KI = 345 nM). Blocks the interaction of ephrin-A1 and ephrin-B1 with all Eph receptors (IC50 = 840 nM - 1.54 µ,M for EphA and 2.6 - 3.74 µ,M for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µ,M), however, it does not affect tyrosine kinase activity of EGF and VEGF receptors. Slightly reduces PC3 cell proliferation without affecting cell cycle or apoptosis. However, it blocks the rounding effect of ephrin-A1-Fc in PC3 cells (IC50 = 6.25 µ,M). Also shown to inhibit angiogenesis in HUVEC (IC50 = 5.2 µ,M) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µ,M, respectively).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.