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HG-10-102-01 LRRK2 inhibitor

Catalog No.B1262
Size Price Stock Qty
10mM (in 1mL DMSO)
$123.00
In stock
5mg
$124.00
In stock
10mg
$219.00
In stock
25mg
$390.00
In stock
50mg
$665.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Chen ZC, Zhang W, et al. "Phosphorylation of amyloid precursor protein by mutant LRRK2 promotes AICD activity and neurotoxicity in Parkinson's disease." Sci Signal. 2017 Jul 18;10(488). pii: eaam6790. PMID:28720718

Quality Control

Chemical structure

HG-10-102-01

Related Biological Data

HG-10-102-01

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Chemical Properties

Cas No. 1351758-81-0 SDF Download SDF
Synonyms N/A
Chemical Name (E)-(4-((5-chloro-6-(methylimino)-1,6-dihydropyrimidin-2-yl)amino)-2-methoxyphenyl)(morpholino)methanone
Canonical SMILES C/N=C(N1)\C(Cl)=CN=C1NC2=CC(OC)=C(C(N3CCOCC3)=O)C=C2
Formula C17H20ClN5O3 M.Wt 377.83
Solubility >18.9mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

HG-10-102-01 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with the IC50 values of 20.3nM and 3.2nM for wild type LRRK2 and LRRK2 [G1019S], respectively [1].

HG-10-102-01 has shown the potent and selective inhibitor of LRRK2 with the IC50 values of 20.3nM, 153.7nM, 95.9nM and 3.2nM for wild type LRRK2, LRRK2 [A2016T], LRRK2 [G2019S+A1016T] and LRRK2 [G1019S], respectively. In addition, HG-10-102-01 has been reported to induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 [G2019S] stably transfected into HEK 293 cells. Moreover, it has been demonstrated that increasing doses of HG-10-102-01 led to similar dephosphorylation of endogenous LRRK2 at Ser910 and Ser935 in HEK293 cells, mouse Swiss 3T3 cells and mouse embryonic fibroblast cells [1].

References:
[1] Choi HG1, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. Epub 2012 Jun 18.