UniPR129 | Ephrin receptor antagonist | Probechem Biochemicals

Chemical Structure : UniPR129

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UniPR129 (UniPR-129, UniPR 129)

货号: 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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生物&药学活性

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).

物理化学性质&存储条件

分子量	576.82
分子式	C36H52N2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. Giorgio C, et al. Biochem Pharmacol. 2018;147:21-29.

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

UniPR129 (UniPR-129, UniPR 129)

生物&药学活性

物理化学性质&存储条件

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UniPR129 (UniPR-129, UniPR 129)

生物&药学活性

物理化学性质&存储条件

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