5.00494
Casein Kinase I Inhibitor VIII
Synonym(s):
Casein Kinase I Inhibitor VIII, 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
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About This Item
Empirical Formula (Hill Notation):
C20H17F2N3O3
CAS Number:
Molecular Weight:
385.36
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
General description
A 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.
A cell-permeable, ATP site-targeting, γ isotype-selective CK1 inhibitor (IC₅₀ = 5 nM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CKIγ
CKIγ
Secondary Target
CKIδ
CKIδ
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Huang, H., et al. 2012. ACS Med. Chem. Lett.3, 1059.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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