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JH-II-127 is a highly selective LRRK2 inhibitor with an IC50 = 6.5 nM.
In vitro: At a concentration of 1 μM, JH-II-127 only inhibited the kinase activities of SmMLCK and CHK2 to greater than 90% of the DMSO control (complete results presented in the Supporting Information). Dose–response analysis revealed inhibition of SmMLCK with an IC50 = 81.3 nM and CHK2 with an IC50 = 27.6 nM.
In vivo: JH-II-127 can inhibit phosphorylation of Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 30 mg/kg.
| Molecular Weight | 416.86 |
| Formula | C19H21ClN6O3 |
| CAS Number | 1700693-08-8 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related LRRK2 Products |
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| GNE-7915
GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor with IC50 and Ki of 9 nM and 1 nM, respectively. |
| GNE-9605
GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM. |
| PF-06447475
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC0 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively. |
| GSK2578215A
GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
| LRRK2-IN-1
LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
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