500494 Casein Kinase I Inhibitor VIII - Calbiochem

500494
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₀H₁₇F₂N₃O₃

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable pyridyl-pyrrolopyridinone compound that acts as an ATP site-targeting, γ isotype-selective CK1 inhibitor (IC50/[ATP] = 5 nM/32 µM, 40 nM/8 µM, and 251 nM/11 µM, respectively, in CK1γ2, CK1δ, and CK1α kinase assays), inhibiting GSK-3β only at much higher concentrations (IC50 = 10.8 µM). Shown to suppress LRP6 phosphorylation in CK1γ2-/LRP6-expressing HEK293 transfectants both in cultures (IC50 = 200 nM) in vitro and in mice (42% reduction 6 h post 50 mg/kg p.o.) in vivo.
      Catalogue Number500494
      Brand Family Calbiochem®
      Synonyms2-(2-((3,4-Difluorophenoxy)methyl)-5-methoxypyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one, CKI Inhibitor VIII, CK1 Inhibitor VIII
      References
      ReferencesHuang, H., et al. 2012. ACS Med. Chem. Lett. 3, 1059.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₀H₁₇F₂N₃O₃
      Chemical formulaC₂₀H₁₇F₂N₃O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCKIγ
      Secondary targetCKIδ
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Casein Kinase I Inhibitor VIII - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Huang, H., et al. 2012. ACS Med. Chem. Lett. 3, 1059.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision31-January-2014 JSW
      Synonyms2-(2-((3,4-Difluorophenoxy)methyl)-5-methoxypyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one, CKI Inhibitor VIII, CK1 Inhibitor VIII
      DescriptionA cell-permeable pyridyl-pyrrolopyridinone compound that acts as an ATP site-targeting, γ isotype-selective CK1 inhibitor (IC50/[ATP] = 5 nM/32 µM, 40 nM/8 µM, and 251 nM/11 µM, respectively, in CK1γ2, CK1δ, and CK1α kinase assays), inhibiting GSK-3β only at much higher concentrations (IC50 = 10.8 µM). Shown to be orally available in mice (Tmax/Cmax = 0.33 h/9.72 µM; t1/2 = 2.7 h; 30 mg/kg p.o.) and significantly suppress LRP6 phosphorylation in CK1γ2-/LRP6-expressing HEK293 transfectants both in cultures (IC50 = 200 nM with 2 h inhibitor incubation) in vitro and in mice (42% reduction 6 h post 50 mg/kg oral dosage) in vivo.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₇F₂N₃O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesHuang, H., et al. 2012. ACS Med. Chem. Lett. 3, 1059.