JH-II-127

Names

[ Name ]:
JH-II-127

[Synonym ]:
Methanone, [4-[[5-chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-4-morpholinyl-
(4-{[5-Chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino}-3-methoxyphenyl)(4-morpholinyl)methanone
JH-II-127

Biological Activity

[Description]:

JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target: LRRK2JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 μM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.

[Related Catalog]:

Signaling Pathways >> Autophagy >> LRRK2

Research Areas >> Neurological Disease

[References]

[1]. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-589.

[Related Small Molecules]

LRRK2-IN-1 | IKK-16 | MLi-2 | PF-06447475 | GNE7915 | GSK2578215A | GNE-9605 | CZC-54252 | GNE-0877 | HG-10-102-01 | CZC 25146

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
581.4±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₂₁ClN₆O₃

[ Molecular Weight ]:
416.861

[ Flash Point ]:
305.4±32.9 °C

[ Exact Mass ]:
416.136353

[ LogP ]:
-0.68

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.701

[ Storage condition ]:
2-8℃

Related Compounds

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