LH846 is a selective inhibitor of casein kinase (CK) 1δ with IC50 of 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α, displays no inhibitory activity at CK2.
LH846 effectively targets CKIδ with an IC50 of 290 nM and shows lesser inhibition towards CKIα and CKIε, with IC50 values of 2.5 μM and 1.3 μM, respectively, while it does not impact CK2. At concentrations of 3 or 10 μM, LH846 blocks CKIδ-mediated phosphorylation of PER1 in HEK293T cells[1].
体外研究
LH846 effectively targets CKIδ with an IC50 of 290 nM and shows lesser inhibition towards CKIα and CKIε, with IC50 values of 2.5 μM and 1.3 μM, respectively, while it does not impact CK2. At concentrations of 3 or 10 μM, LH846 blocks CKIδ-mediated phosphorylation of PER1 in HEK293T cells[1].
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