化合物SL-327 T2708

Product Introduction
Bioactivity


英文名: SL327

描述: SL327 是能通过血脑屏障运输的选择性 MEK1/2 抑制剂，IC50 分别为 0.18 和 0.22 μM。

激酶实验: The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25 mM Hepes, 1 mM EDTA, 1 mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4 mM leupeptin, 4 mg/mL aprotinin, and 0.3 mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120 μg) are incubated at room temperature for 2 h with the indicated concentrations of Pifithrin-α in the presence of 3 nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice, resuspended in 0.2 mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone[2].

体外活性: 30 mg/Kg SL327明显损害小鼠空间学习记忆.50 mg/kg SL327可以透过血-脑屏障,通过抑制MAPK/ERK磷酸化而抑制条件性恐惧.

体内活性: SL327对多种其他包括PKA,PKC或CamKII的激酶没有抑制效果。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 33.5 mg/mL (100 mM)
Ethanol : 16.8 mg/mL (50 mM)


关键字: Mitogen-activated protein kinase kinase | MEK | inhibit | SL327 | Inhibitor | MAPKK | MAP2K

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相关库: Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | Reprogramming Compound Library | MAPK Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compound Library

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