Chemical Structure : UniPR129
CAS No.:
1639159-47-9
UniPR129
(UniPR 129)
Catalog No.: PC-20805Not For Human Use, Lab Use Only.
UniPR129 is a potent, selective Eph/ephrin antagonist, competitively disrupts Eph2A-ephrin-A1 binding (IC50=945 nM, Ki = 345 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
UniPR129 is a potent, selective Eph/ephrin antagonist, competitively disrupts Eph2A-ephrin-A1 binding (IC50=945 nM, Ki = 345 nM).
UniPR129 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).
UniPR129 inhibits EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µM), does not affect tyrosine kinase activity of EGF and VEGF receptors.
UniPR129 inhibits angiogenesis in HUVEC (IC50 = 5.2 µM) and reduces ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µM, respectively).
Physicochemical Properties
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M.Wt
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576.82
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Formula
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C36H52N2O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C(O)C[C@@H](NC(CC[C@H]([C@H]1CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)C)=O)CC5=CNC6=C5C=CC=C6
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References
1. Giorgio C, et al. Biochem Pharmacol. 2018;147:21-29.
2. Hassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm. 171, 5195.
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