5.00713

EphA Antagonist

• Synonym(e): EphA Antagonist, Rtk2 Antagonist, Rtk1 Antagonist, 4-(2,5-dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, EphA2 Antagonist, EphA4 Antagoinst, Ephrin Receptor Antagonist
• Empirische Formel (Hill-System): C₁₃H₁₃NO₃
• CAS-Nummer: 674782-30-0
• Molekulargewicht: 231.25
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥95% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: 3 μM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: orange
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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 (K_i = 6-10 and 11-14 µM against ephrin-A5 binding to EphA4 and EphA2, respectively), 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 0.1 µg/mL ephrin-A1-Fc fusion-induced EphA2 phosphorylation in COS7 (by 92% at 200 µM) and 0.5 µg/mL ephrin-A5-Fc fusion-induced EphA4 phosphorylation in HT22 neuronal cultures (by 42% and 79% respectively, at 300 and 400 µM) without any cytotoxicity (up to 400 µM and 3 days in HT22 cultures). Also effective toward chicken and zebrafish EphA4 orthologs as evidenced by its efficacy in preventing 1 µg/mL ephrin-A5-Fc-induced growth cone collapse of neurons in 6-d chicken embryo retina (by 100% at 400 µM) ex vivo and in fully rescuing human mutant SOD-1 A4V transgene-induced axonopathy in zebrafish embryos (500 µM; treatment period from 6 to 30 hpf) in vivo.

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 200 µM) and ephrin-A5-induced EphA4 phosphorylation (by 79% at 400 µM) in cultures in vitro and prevent ephrin-A5-induced growth cone collapse of neurons in 6-d chicken embryo retina (by 100% at 400 µM) ex vivo, as well as rescue human mutant SOD-1 A4V transgene-induced axonopathy in zebrafish embryos (500 µM from 6 to 30 hpf) in vivo.

Biochem./physiol. Wirkung

Cell permeable: no

Primary Target
EphA

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

Van Hoecke, A., et al. 2012. Nat. Med.18, 1418.
Noberini, R., et al. 2008. J. Biol. Chem.283, 29461.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable