GSK2578215A
作者：齐岳
发布时间：2023-09-12
09:13:30
点击数：
产品名称：GSK2578215A
产品描述：
| 产品描述 | GSK2578215A is a potent and selective LRRK2 kinase inhibitor. |
| 靶点活性 | LRRK2 (WT):10.9 nM, LRRK2 (G2019S):8.9 nM |
| 体外活性 | 100 mg/kg i.p. GSK2578215A抑制小鼠脾脏和肾中Ser910 和Ser935磷酸化,但在大脑中没有作用. |
| 体内活性 | SH-SY5Y细胞中,GSK2578215A通过改变自噬体 - 溶酶体融合来损害自噬流,并且通过诱导Drp-1介导的线粒体分裂和线粒体衍生的ROS信号传导诱导线粒体自噬。GSK2578215A在稳定转染到HEK293细胞中的野生型LRRK2和LRRK2 [G2019S]中诱导对Ser910和Ser935磷酸化的剂量依赖性抑制,并诱导小鼠Swiss 3T3细胞中内源性LRRK2的类似的剂量依赖性Ser910和Ser935去磷酸化。 |
| 激酶实验 | PFV integration assay: For quantitative strand transfer assays, donor DNA substrate is formed by annealing HPLC grade oligonucleotides 5′-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA and 5′-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC. Reactions (40 μL) contains 0.75 μM PFV IN, 0.75 μM donor DNA, 4 nM (300 ng) supercoiled pGEM9-Zf(?) target DNA, 125 mM NaCl, 5 mM MgSO4, 4 μM ZnCl2, 10 mM DTT, 0.8% (vol/vol) DMSO, and 25 mM BisTris propane–HCl, pH 7.45. Raltegravir is added at indicated concentrations. Reactions are initiated by addition of 2 μL PFV IN diluted in 150 mM NaCl, 2 mM DTT, and 10 mM Tris-HCl, pH 7.4, and stopped after 1 hour at 37 °C by addition of 25 mM EDTA and 0.5% (wt/vol) SDS. Reaction products, deproteinized by digestion with 20 μg proteinase K for 30 minutes at 37 °C followed by ethanol precipitation, are separated in 1.5% agarose gels and visualized by staining with ethidium bromide. Integration products are quantified by quantitative real-time PCR, using Platinum SYBR Green qPCR SuperMix and three primers: 5′-CTACTTACTCTAGCTTCCCGGCAAC, 5′-TTCGCCAGTTAATAGTTTGCGCAAC, and 5′-GACTCACTATAGGGCACGCGT. PCR reactions (20 μL) contained 0.5 μM of each primer and 1 μL diluted integration reaction product. Following a 5-min denaturation step at 95 °C, 35 cycles are carried out in a CFX96 PCR instrument, using 10 seconds denaturation at 95 °C, 30 seconds annealing at 56 °C and 1 minutes extension at 68 °C. Standard curves are generated using serial dilutions of WT PFV IN reaction in the absence of INSTI. |
| 别名 | 5-(2-氟-4-吡啶基)-2-(苯基甲氧基)-N-3-吡啶基苯甲酰胺 |
| 分子量 | 399.42 |
| 分子式 | C24H18FN3O2 |
| CAS No. | 1285515-21-0 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 39.9 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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