Background:

LH846 is an inhibitor of casein kinases with IC50 values of 290nM, 2.5μM and 1.3μM against CKIδ, CKIα and CKIε, respectively [1].

As a small inhibitor of casein kinase, LH846 is developed for the treatment of the diseases that have an underlying circadian disorder. LH846 is previously screened out from a cell-based assay using human U2OS cells. It affects the circadian rhythm and lengthens the period (10h) at concentration of 8μM. LH846 can inhibit the activity of CKIδ, CKIα and CKIε with IC50 values of 290nM, 2.5μM and 1.3μM, respectively. The specific target of it is CKIδ. When treated with a panel of about 50 kinases, LH846 exerts potent inhibition against CKIδ and less potent effects on CKIα and ROCK2. CK2 is not sensitive to LH846 [1].

参考文献:
[1] Lee J W, Hirota T, Peters E C, et al. A small molecule modulates circadian rhythms through phosphorylation of the period protein. Angewandte Chemie, 2011, 123(45): 10796-10799.