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HG-10-102-01

Chemical Structure : HG-10-102-01

CAS No.: 1351758-81-0

HG-10-102-01

Catalog No.: PC-22264Not For Human Use, Lab Use Only.

HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 and LRRK2 G2019S mutant with IC50 of 20.3 nM and 3.2 nM, respectively.

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Biological Activity

HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 and LRRK2 G2019S mutant with IC50 of 20.3 nM and 3.2 nM, respectively.
HG-10-102-01 is capable of inhibiting LRRK2 phosphorylation in mouse brain.
HG-10-102-01 maintains inhibition of the A2016T mutation (IC50=153.7 nM), which induces dramatic resistance to LRRK2-IN-1.
HG-10-102-01 (0.03-1 uM) induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells.
HG-10-102-01 also induced dephosphorylation of Ser910 and Ser935 at a concentration of 1-3 μM in the drug-resistant LRRK2[A2016T + G2019S] and LRRK2[A2016T] mutants.
HG-10-102-01 is capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.

Physicochemical Properties

M.Wt 377.83
Formula C17H20ClN5O3
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

(4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone

References

1. Choi HG, et al. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662.

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