Eph Receptor Antagonist, UniPR129

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; K_I = 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; K_I = 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.

Cell permeable: yes

Primary Target
Eph Receptors

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Hassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm.171, 5195.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany