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GNE⁻⁷915

CAS No. : 1351761-44-8

MCE 国际站：GNE⁻⁷915

产品活性：GNE⁻⁷915是高效选择性，可渗透大脑的LRRK2抑制剂，IC₅₀值为9 nM。

研究领域：Autophagy

作用靶点：LRRK2

In Vitro: Maintaining the methoxy/fluoro arrangement at C-2′/C-5′ and varying aminoalkyl R1 substitution resultes in single-digit nanomolar LRRK2 cellular activities for GNE⁻⁷915 and compound 19. Expanded Invitrogen kinase profiling (187 kinases) at 0.1 µM for both GNE⁻⁷915 (100-fold over LRRK2 Ki) and 19 (250-fold over LRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverX KinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed for GNE⁻⁷915 at 0.1 µM. Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE⁻⁷915. Cerep receptor profiling, including expanded brain panels, suggestes that GNE⁻⁷915 and 19 only inhibite 5-HT_2B with >70% inhibition at 10 µM. GNE⁻⁷915 and 19 are confirmed to be moderately potent 5-HT_2B antagonists in vitro functional assays.

相关产品：Bioactive Compound Library Plus | Kinase Inhibitor Library | Autophagy Compound Library | CZC-54252 | GNE-9605 | CZC-25146

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