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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.
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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 |
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| PF-4800567
PF-4800567 is a selective, ATP competitive casein kinase 1ε inhibitor with IC50 values of 32 and 711 nM for CK1ε and CK1δ respectively. |
| D4476
D4476 is a selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) with IC50 of 0.3 µM and 0.5 µM, respectively. |
| TTP 22
TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM. |
| TBB
TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively). |
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