A pyrrolyl benzoic acid that effectively competes against ephrin-B3 for EphA4 binding as well as against ephrin-A1/-A2/-A3/-A5 for EphA2 and EphA4 binding by targeting EphA2/A4 high affinity ephrin-binding pocket in a reversible manner, exhibiting much reduced or no potency against ephrin-A4 for EphA2/EphA4 binding, ephrin-A5 for EphA3/A5/A6/A7 binding, ephrin-B2 for B1/B2/B3/B4/B6 binding, or ephrin-B2 for EphA4 binding. Shown to inhibit ephrin-A1-induced EphA2 phosphorylation (by 92% at 200uM) and ephrin-A5-induced EphA4 phosphorylation (by 79% at 400uM) in cultures in vitro and prevent ephrin-A5-induced growth cone collapse of neurons in 6-d chicken embryo retina (by 100% at 400uM) ex vivo, as well as rescue human mutant SOD-1 A4V transgene-induced axonopathy in zebrafish embryos (500uM from 6 to 30hpf) in vivo.
Solubility:DMSO
Primary Target:EphA
Primary Target IC50:3 micro
Molar Mass:231.25
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
