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Lu AF58786

Chemical Structure : Lu AF58786

CAS No.: 1632368-13-8

Lu AF58786

Catalog No.: PC-49826Not For Human Use, Lab Use Only.

Lu AF58786 is a potent and selective LRRK2 inhibitor with IC50 of 12 nM, 19 nM and 93 nM for LRRK2 WT, LRRK2-G2019S and LRRK2-A2016T in cell-based assays, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Lu AF58786 is a potent and selective LRRK2 inhibitor with IC50 of 12 nM, 19 nM and 93 nM for LRRK2 WT, LRRK2-G2019S and LRRK2-A2016T in cell-based assays, respectively.
Lu AF58786 is a potent inhibitor of LRRK2 and G2019S that also engages alanine at position 2016 in LRRK2.
Lu AF58786 selectively inhibits LRRK2 in human PBMCs, shows high selectivity in human PBMCs using the ActivX KiNativ assays at 100 nM.|
Lu AF58786 showed inhibition of LRRK2-Ser935 phosphorylation in human PBMCs.
Lu AF58786 inhibited phosphorylation of LRRK2, Rab10 and Rab12 in cultured and immune stimulated human PBMCs.

Physicochemical Properties

M.Wt 328.38
Formula C19H16N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-((1-methyl-1H-pyrazol-3-yl)amino)-4-(m-tolyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile

References

1. Kenneth Thirstrup, et al. Sci Rep. 2017 Aug 31;7(1):10300.

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