General description
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; KI = 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; KI = 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 Actions
Cell permeable: yes
Primary Target
Eph Receptors
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Hassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm.171, 5195.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 576.81. Empirical Formula: C36H52N2O4. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. potency: 945 . nM IC50. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 50 . mg/mL. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51181915
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5338710001
