An inhibitor of wild-type and mutant forms of LRRK2; inhibits WT LRRK2

JH-II-127 – 1 mg

Brand:
Cayman
CAS:
1700693-08-8
Storage:
-20
UN-No:
Non-Hazardous - /

JH-II-127 is an orally bioavailable inhibitor of wild-type (WT) and mutant forms of leucine-rich repeat kinase 2 (LRRK2).{47651} It inhibits WT LRRK2, as well as LRRK2 containing the G2019S and A2016T substitution mutations (IC50s = 6.6, 2.2, and 47.7 nM, respectively), which are present in certain patients with Parkinson’s disease, but not LRRK2 containing both mutations (IC50 = 3,080 nM). JH-II-127 (0.1-0.3 µM) inhibits phosphorylation of the serines at positions 910 and 935 of WT LRRK2 and LRRK2G2019S in vitro. It also inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney when administered at a dose of 30 mg/kg.  

 

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SKU: 22905 - 1 mg Category:

Description

An inhibitor of wild-type and mutant forms of LRRK2; inhibits WT LRRK2, LRRK2G2019S, and LRRK2A2016T (IC50s = 6.6, 2.2, and 47.7 nM, respectively) but not LRRK2 containing both mutations (IC50 = 3,080 nM); inhibits phosphorylation of Ser910 and Ser935 of WT LRRK2 and LRRK2G2019S in vitro; inhibits Ser935 phosphorylation in vivo in mouse brain, spleen, and kidney at 30 mg/kg

Formal name: [4-[[5-chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-4-morpholinyl-methanone

Synonyms: 

Molecular weight: 416.9

CAS: 1700693-08-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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