1700693-08-8

1700693-08-8 structure

Name: JH-II-127
Chemical Name: (4-{[5-Chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino}-3-methoxyphenyl)(4-morpholinyl)methanone
CAS Number: 1700693-08-8
Molecular Formula: C₁₉H₂₁ClN₆O₃
Molecular Weight: 416.861
Catalog: Signaling Pathways Autophagy LRRK2
Create Date: 2018-02-01 19:20:58
Modify Date: 2024-01-27 00:18:22
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.

Name	(4-{[5-Chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino}-3-methoxyphenyl)(4-morpholinyl)methanone
Synonyms	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

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.