ML-18
产品说明书
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同义名 : | - |
| CAS号 : | 1422269-30-4 | |
| 货号 : | A708758 | |
| 分子式 : | C32H35N5O5 | |
| 纯度 : | 98%+ | |
| 分子量 : | 569.65 | |
| MDL号 : | MFCD30182327 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Bombesin receptor subtype (BRS)-3 is an orphan G-protein coupled receptor (GPCR) whose role in normal physiology is unknown due to a lack of specific agonists and antagonists. ML-18, an antagonist of BRS-3 with IC50 of 4.8 μM, is used to inhibit lung cancer growth. Addition of 16 μM ML-18 antagonized the ability of 10 nM BA1 to increase cytosolic Ca2+ in lung cancer cells. Subsequent addition of 1 μM BA1 increased the cytosolic Ca2+ strongly indicating that ML-18 is a reversible nonpeptide BRS-3 antagonist. The increase in FAK, ERK and EGFR tyrosine phosphorylation caused by 0.1 μM BA1 was significantly inhibited by 16 μM ML-18. The results indicate that ML-18 in a dose-dependent manner decreases lung cancer FAK, ERK and EGFR tyrosine phosphorylation that is regulated by BRS-3. Further, proliferation of NCI-H1299 cells transfected with BRS-3 was moderately and strongly inhibited by 16 and 48 μM ML-18. In the clonogenic assay, 1.6 μM ML-18 significantly reduced the NCI-H727 colony number. Finally, 10 nM MK5046 (BRS-3 agonist) stimulated and increase in cytosolic calcium of NCI-H1299 cells transfected with BRS-3 and this increase was inhibited by ML-18 at 16 μM[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.76mL 0.35mL 0.18mL |
8.78mL 1.76mL 0.88mL |
17.55mL 3.51mL 1.76mL |
| 参考文献 |
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