MK-1468 | LRRK2 inhibitor | Probechem Biochemicals

Chemical Structure : MK-1468

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MK-1468 (MK1468)

货号: PC-21271Not For Human Use, Lab Use Only.

MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.

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生物&药学活性

MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.
MK-1468 demonstrates near-equipotent activity for LRRK2 (G2019S) and wild-type LRRK2.
MK-1468 is >100-fold selective against 265 off-target kinases tested, and >1000-fold selectivity against a panel of 117 functional, enzyme, and radioligand binding assays screened (Cerep, Panlabs).
MK-1468 inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in the rat brain, orally active.

物理化学性质&存储条件

分子量	501.02
分子式	C26H33ClN4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-N-(7-chloro-6-(4-((3R,4R)-4-hydroxy-3-methyltetrahydrofuran-3-yl)piperazin-1-yl)isoquinolin-3-yl)-6-oxaspiro[2.5]octane-1-carboxamide

参考文献

1. Kattar SD, et al. J Med Chem. 2023 Oct 20. doi: 10.1021/acs.jmedchem.3c01486.

MK-1468 (MK1468)

生物&药学活性

物理化学性质&存储条件

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MK-1468 (MK1468)

生物&药学活性

物理化学性质&存储条件

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