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500494 Casein Kinase I Inhibitor VIII - Calbiochem

A cell-permeable, ATP site-targeting, γ isotype-selective CK1 inhibitor (IC₅₀ = 5 nM).

Casein Kinase I Inhibitor VIII - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(2-((3,4-Difluorophenoxy)methyl)-5-methoxypyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one, CK1 Inhibitor VIII, CKI Inhibitor VIII

Primary Target: CKIγ
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₀H₁₇F₂N₃O₃

Products

Catalog NumberPackaging Qty/Pack
5.00494.0001 Glass bottle 10 mg
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, CK1 Inhibitor VIII, CKI 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
Global Trade Identification Number
Catalog Number GTIN
5.00494.00014055977245592

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, CK1 Inhibitor VIII, CKI 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 Protect from light
+2°C to +8°C
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.