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化驗
≥98% (HPLC)
品質等級
形狀
solid
效力
945 nM IC50
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
off-white
溶解度
DMSO: 50 mg/mL
儲存溫度
−20°C
一般說明
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.
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.
生化/生理作用
Cell permeable: yes
Primary Target
Eph Receptors
Eph Receptors
Reversible: yes
包裝
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他說明
Hassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm.171, 5195.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
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