Eph Receptor Antagonist, UniPR129-Calbiochem

半岛bd体育手机客户端 说明

一般描述

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 ?M for EphA and 2.6 - 3.74 ?M for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC₅₀= 5 ?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 ?M). Also shown to inhibit angiogenesis in HUVEC (IC₅₀= 5.2 ?M) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC₅₀= 26.3 and 18.4 ?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; K_I= 345 nM). Blocks the interaction of ephrin-A1 and ephrin-B1 with all Eph receptors (IC₅₀= 840 nM - 1.54 ?M for EphA and 2.6 - 3.74 ?M for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC₅₀= 5 ?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 ?M). Also shown to inhibit angiogenesis in HUVEC (IC₅₀= 5.2 ?M) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC₅₀= 26.3 and 18.4 ?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.

生化/生理作用

Cell permeable: yes
Primary Target
Eph Receptors
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

基本信息

半岛bd体育手机客户端 性质

安全信息