
簡(jiǎn)要描述:GSK2578215A 1285515-21-0GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
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Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 1285515-21-0 |
|---|---|---|---|
| 分子式 | C24H18FN3O2 | 純度 | >98% |
| 分子量 | 399.42 | 貨號(hào) | abs47027961 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent and selective | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
GSK2578215A 1285515-21-0
| 產(chǎn)品描述 | |
| 描述 | GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
| 純度 | >98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | LRRK2-kinase inhibitor |
| 外觀 | white to beige powder |
| 可溶性/溶解性 | DMSO : 50 mg/mL (125.18 mM) |
| 生物活性 | |
| 靶點(diǎn) | LRRK2 (G2019S),LRRK2 (WT) |
| In vitro(體外研究) | GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 stably transfected into HEK293 cells, and induces similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells. In SH-SY5Y cells, GSK2578215A impairs the autophagy flux by altering autophagosome–lysosome fusion, and induces mitophagy though induction of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. |
| In vivo(體內(nèi)研究) | In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain. |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | NeuroscienceDiseases NeuroscienceNeurology processNeurodegenerative diseaseParkinson's diseaseSynuclein Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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