5.33871

Eph Receptor Antagonist, UniPR129

• Synonym(e): Eph Receptor Antagonist, UniPR129, (S)-3-((R)-4-((3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)-4-(1H-indol-3-yl)butanoic acid, Eph Inhibitor, UniPR129
• Empirische Formel (Hill-System): C₃₆H₅₂N₂O₄
• Molekulargewicht: 576.81
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 945 nM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Eph Receptors

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

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable