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SML2569

Sigma-Aldrich

JH-II-127

≥98% (HPLC)

Synonym(s):

[4-[[5-Chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-4-morpholinylmethanone

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About This Item

Empirical Formula (Hill Notation):
C19H21ClN6O3
CAS Number:
1700693-08-8
Molecular Weight:
416.86
MDL number:
MFCD29472241
UNSPSC Code:
12352200
NACRES:
NA.77
Pricing and availability is not currently available.

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

Clc1c2c(nc([nH]c2NC)Nc3c(cc(cc3)C(=O)N4CCOCC4)OC)nc1

InChI

1S/C19H21ClN6O3/c1-21-16-15-12(20)10-22-17(15)25-19(24-16)23-13-4-3-11(9-14(13)28-2)18(27)26-5-7-29-8-6-26/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24,25)

Biochem/physiol Actions

JH-II-127 is an orally available, brain penetrant, potent and selective inhibitor of both wild-type and G2019S mutant Leucine-rich repeat kinase 2 (LRRK2). JH-II-127 inhibits phosphorylation of the Ser910 and Ser935 of both wild-type and G2019S mutant LRRK2. It causes complete inhibition of LRRK2 in mouse brain at 100 mg/kg.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Farzaneh Atashrazm et al.
Clinical pharmacology : advances and applications, 8, 177-189 (2016-11-02)
Major advances in understanding how genetics underlies Parkinson's disease (PD) have provided new opportunities for understanding disease pathogenesis and potential new targets for therapeutic intervention. One such target is leucine-rich repeat kinase 2 (LRRK2), an enigmatic enzyme implicated in both
John M Hatcher et al.
ACS medicinal chemistry letters, 6(5), 584-589 (2015-05-26)
Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here we report a 2-anilino-4-methylamino-5-chloropyrrolopyrimidine, JH-II-127 (18), as a potent and selective inhibitor of both

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