DC Chemicals · Product datasheet

JH-II-127 — Datasheet

CAT. NO. DC8379

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ParameterValue
Chemical Name[4-[[5-Chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
CAS No.1700693-08-8
SynonymsJH-II-127;(4-((5-chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone;[4-[[5-Chloranyl-4-(Methylamino)-7~{h}-Pyrrolo[2,3-D]pyrimidin-2-Yl]amino]-3-Methoxy-Phenyl]-Morpholin-4-Yl-Methanone;BCP16207;SB19025;AK473658;A15777;A1K;[4-[[5-chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amin;[4-[[5-Chloro-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-yl
FormulaC19H21ClN6O3
M.Wt416.8614
SMILESClC1=C([H])N([H])C2=C1C(N([H])C([H])([H])[H])=NC(=N2)N([H])C1C([H])=C([H])C(=C([H])C=1OC([H])([H])[H])C(N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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.

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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