Biological Activity
Selective inhibitor of casein kinase (CK) 1δ (IC50 values are 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α); displays no inhibitory activity at CK2. Inhibits CK1δ-dependent phosphorylation and degradation of PER1 protein. Shown to lengthen the circadian period in U2OS cells, with minimal effect on amplitude.
Compound Libraries
LH 846 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 316.81 |
| Formula | C16H13ClN2OS |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 639052-78-1 |
| PubChem ID | 851474 |
| InChI Key | DYHAMRNAHTWYKY-UHFFFAOYSA-N |
| Smiles | O=C(CC3=CC=CC=C3)NC(S2)=NC1=C2C=C(C)C(Cl)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.68 | 100 | |
| ethanol | 1.58 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 316.81. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.16 mL | 15.78 mL | 31.56 mL |
| 5 mM | 0.63 mL | 3.16 mL | 6.31 mL |
| 10 mM | 0.32 mL | 1.58 mL | 3.16 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lee et al (2011) A small molecule modulates circadian rhythms through phosphorylation of the period protein. Agnew Chem.Int.Ed.Engl. 50 10608 PMID: 21954091
Keywords: LH 846, supplier, LH846, casein, kinase, I, CK1, CK1d, CK1delta, CK1δ, selective, inhibitors, inhibits, circadian, rhythm, clock, Casein, Kinase, 1, Casein, Kinase, 1, Tocris Bioscience
