Chemical Structure : MK-1468
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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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.
分子量 | 501.02 | |
分子式 | C26H33ClN4O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Kattar SD, et al. J Med Chem. 2023 Oct 20. doi: 10.1021/acs.jmedchem.3c01486.
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