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LH846

Cat. No. M8957
LH846 Structure
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10mg USD 100 In stock
50mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 316.81
Formula C16H13ClN2OS
CAS Number 639052-78-1
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

A small molecule modulates circadian rhythms through phosphorylation of the period protein.
Lee JW, et al. Angew Chem Int Ed Engl. 2011 Nov 4;50(45):10608-11. PMID: 21954091.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LH846 supplier, Casein Kinase, inhibitors

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