assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
clearpale yellow
shipped in
wet ice
Quality Level
General description
A cell-permeable, potent, reversible, ATP-competitive and highly selective inhibitor of IKK-2 (IC50 ~3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2) that also displays anti-inflammatory properties. Specificity has been reported using a panel of 31 additional kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC50 >200 µM). Shown to specifically block NF-κB-dependent gene expression, but not MAP kinase pathways, in stimulated RASF synovial fibroblast cells. Does not inhibit the phosphorylation and activation of the IKK complex.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IKK-2
IKK-2
Product competes with ATP.
Reversible: yes
Target IC50: ~ 3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2
Packaging
Packaged under inert gas
Physical form
A 25 mM (1 mg/178 µl) solution of IKK-2 Inhibitor, SC-514 (Cat. No. 401479) in DMSO.
Preparation Note
Following initial use, aliquot and refrigerate (4°C).
Other Notes
Baxter, A., et al. 2004 Bioorg. Med. Chem. Lett.14, 2817.
Kishore, N., et al. 2003. J. Biol. Chem.278, 32861.
Kishore, N., et al. 2003. J. Biol. Chem.278, 32861.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
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