Biochem/physiol Actions

LH846 is a potent and selective inhibitor of the known clock regulatory kinase Casein Kinase CK1δ, with an IC₅₀ of 290 nm, compared to an IC₅₀ of 2.5 μm for CKIα , 1.3 μm for CKIε, and minimal effect on CK2 and 50 other kinases tested. Circadian rhythym has been studied for a long time for things such as jet lag rhythym related disorders, but more recently it has beencome apparent that clock dysfunction can contribute to a variety of pathologies including circadian sleep disorders, cardiovascular disease, cancer, and metabolic disease, so studies of clock regulating enzymes have increased. LH846 increased circadian period by 10 hours in human U2OS cells.