GSK2578215A
作者：齊岳
發(fā)布時(shí)間：2023-09-12
09:13:30
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：GSK2578215A
產(chǎn)品描述：
| 產(chǎn)品描述 | GSK2578215A is a potent and selective LRRK2 kinase inhibitor. |
| 靶點(diǎn)活性 | LRRK2 (WT):10.9 nM, LRRK2 (G2019S):8.9 nM |
| 體外活性 | 100 mg/kg i.p. GSK2578215A抑制小鼠脾臟和腎中Ser910 和Ser935磷酸化,但在大腦中沒(méi)有作用. |
| 體內(nèi)活性 | SH-SY5Y細(xì)胞中,GSK2578215A通過(guò)改變自噬體 - 溶酶體融合來(lái)?yè)p害自噬流,并且通過(guò)誘導(dǎo)Drp-1介導(dǎo)的線粒體分裂和線粒體衍生的ROS信號(hào)傳導(dǎo)誘導(dǎo)線粒體自噬。GSK2578215A在穩(wěn)定轉(zhuǎn)染到HEK293細(xì)胞中的野生型LRRK2和LRRK2 [G2019S]中誘導(dǎo)對(duì)Ser910和Ser935磷酸化的劑量依賴(lài)性抑制,并誘導(dǎo)小鼠Swiss 3T3細(xì)胞中內(nèi)源性LRRK2的類(lèi)似的劑量依賴(lài)性Ser910和Ser935去磷酸化。 |
| 激酶實(shí)驗(yàn) | 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. |
| 別名 | 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 |
存儲(chǔ)
| 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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