1632368-13-8
Chemical Structure
Lu AF58786
- CAS No.: 1632368-13-8
- Formula:C19H16N6
- Molecular Weight:328.37
IUPAC Name: 6-((1-methyl-1H-pyrazol-3-yl)amino)-4-(m-tolyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
InChIKey: IQBHNQCIUDQGPV-UHFFFAOYSA-N
SMILES: N#CC1=CNC2=NC(NC3=NN(C)C=C3)=CC(C4=CC(C)=CC=C4)=C12
Biological Activity: Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC50 of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC50s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research[1][2].
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Lu AF58786 | Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC50 of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC50s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research. | |||||||||||||||||||||
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- [1]. Thirstrup K, et al. Selective LRRK2 kinase inhibition reduces phosphorylation of endogenous Rab10 and Rab12 in human peripheral mononuclear blood cells. Sci Rep. 2017 Aug 31;7(1):10300. [Content Brief]
- [2]. Williamson DS, et al. Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1). J Med Chem. 2017 Nov 9;60(21):8945-8962. [Content Brief]
Keywords
