产品说明书
2-Bromo-4'-hydroxyacetophenone
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同义名 : | 2-溴-4'-羟基苯乙酮 ;PTP Inhibitor I;4-Hydroxyphenacyl bromide;Protein Tyrosine Phosphatase Inhibitor I;SHP-1 Inhibitor II;α-Bromo-4-hydroxyacetophenone |
| CAS号 : | 2491-38-5 | |
| 货号 : | A172579 | |
| 分子式 : | C8H7BrO2 | |
| 纯度 : | 98% | |
| 分子量 : | 215.044 | |
| MDL号 : | MFCD00072424 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 250 mg/mL(1162.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | PTP Inhibitor I is a photoreversible covalent Inhibitor of PTP (Protein Tyrosine Phosphatases) with Ki value of 42μM for PTP1B. PTP Inhibitor I could bind to the PTP active site as a phosphotyrosine mimetic. Its phenyl ring could engage in hydrophobic interactions with the protein as the phenyl ring of a substrate does, and the electron-rich halogen atom could mimic the negatively charged phosphate oxyanions. Binding of PTP Inhibitor I to the PTP active site in such a manner would place the R-carbon, which is highly susceptible to nucleophilic attack, next to the catalytic cysteine. An SN2 reaction between 1 and the cysteine thiol would result in the formation of a covalent enzyme-inhibitor adduct through a stable thioether linkage and loss of phosphatase activity. Treatment with PTP Inhibitor I>300μM resulted in the hyperphosphorylation of a protein at 110 kDa in human B cells post 3min, consistent with inhibition of a PTP(s) which normally dephosphorylates this protein. Also it decreased the phosphorylation level of a 50 kDa protein at concentrations as low as 30μM. | ||
| 作用机制 | PTP Inhibitor I could bind to the PTP active site as a phosphotyrosine mimetic.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.65mL 0.93mL 0.47mL |
23.25mL 4.65mL 2.33mL |
46.50mL 9.30mL 4.65mL |
| 参考文献 |
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