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PTP inhibitor 1

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Chemical Structure| 2632-13-5 同义名 : α-溴代-4-甲氧基苯乙酮 ;α-Bromo-4’-methoxyacetophenone;NSC 129010;Protein Tyrosine Phosphatase Inhibitor II;4-Methoxyphenacyl bromide;ω-Bromo-4’-methoxyacetophenone;4-(Bromoacetyl)anisole;PTP Inhibitor II
CAS号 : 2632-13-5
货号 : A356070
分子式 : C9H9BrO2
纯度 : 98%
分子量 : 229.07
MDL号 : MFCD00000201
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(458.37 mM)，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

H2O: 1 mg/mL(4.37 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 PTP Inhibitor II is a photoreversible covalent Inhibitor of PTP (Protein Tyrosine Phosphatases) with Ki value of 128μM for SHP-1(ΔSH2). PTP Inhibitor II 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 II 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.
作用机制 PTP Inhibitor II could bind to the PTP active site as a phosphotyrosine mimetic.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.37mL

0.87mL

0.44mL

21.83mL

4.37mL

2.18mL

43.65mL

8.73mL

4.37mL
参考文献

[1]α-Haloacetophenone Derivatives As Photoreversible Covalent Inhibitors of Protein Tyrosine Phosphatases