LH846 |
| Catalog No.GC17466 |
Le LH846 est un inhibiteur sélectif de CKIδ, avec une IC50 de 290 nM, et inhibe moins puissamment CKIα et CKIε, avec des IC50 de 2,5 μM et 1,3 μM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 639052-78-1
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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.
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