LH846 is a selective inhibitor of casein kinase with IC50 values of 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α, respectively. LH846 (3 or 10 μM) inhibits CKIδ-dependent phosphorylation of PER1 protein in HEK293T cells and to lengthen the circadian period in U2OS cells.
 |
Source | Angew Chem Int Ed Engl (2011 Nov). Figure 4. LH846 |
| Method | Western blot | |
| Cell Lines | HEK293T cells | |
| Concentrations | 3 or 10 μM | |
| Incubation Time | 7 h | |
| Results | Coexpression of PER1 with CKIδ resulted in a mobility shift and lower abundance of PER1 protein. Treatment with LH846 reduced the PER1 mobility shift and PER1 clearance in a dose-dependent manner, indicating that CKIδ-dependent phosphorylation and subsequent degradation of PER1 protein is inhibited by LH846 treatment. |
| Cell Experiment | |
|---|---|
| Cell lines | HEK293T cells |
| Preparation method | HEK293T cells were reversely transfected on 12-well plates by Lipofectamine 2000 with expression vectors for C-terminally 3XFlag-tagged PER1 protein and N-terminally HA-tagged CKIδ. The cells were treated with 3 or 10 μM LH846 or 0.1% DMSO for 7 h, and a part of the cell extract was analyzed by Western blot to detect the PER1-Flag protein. |
| Concentrations | 3 or 10 μM |
| Incubation time | 7 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 316.81 |
| Formula | C16H13ClN2OS |
| CAS Number | 639052-78-1 |
| Solubility (25°C) | DMSO: ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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