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 µM for EphA and 2.6 - 3.74 µM for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µM), 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 µM). Also shown to inhibit angiogenesis in HUVEC (IC50 = 5.2 µM) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µM, 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 µM for EphA and 2.6 - 3.74 µM for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µM), 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 µM). Also shown to inhibit angiogenesis in HUVEC (IC50 = 5.2 µM) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µM, 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.
Acciones bioquímicas o fisiológicas
Cell permeable: yes
Primary Target Eph Receptors
Reversible: yes
Envase
Packaged under inert gas
Advertencia
Toxicity: Standard Handling (A)
Reconstitución
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Otras notas
Hassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm.171, 5195.
Información legal
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
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