General description
A cell-permeable IKK-2 inhibitor that selectively blocks IκBα phosphorylation (IC50 ~250 nM) and prevents the induction of NF-κB p65 nuclear translocation. Reported to suppress neoplastic proliferation of mast cells with constitutively activated c-kit receptor. Shown to offer cardioprotection by reducing IL-1β and MCP-1 production (IC50<1 µM) in cardiomyocytes, and ameliorate insulin resistance in diabetic KKAy mice by regulating adiponectin release.
A cell-permeable salicylamide compound that acts as an IKK-2 inhibitor by selectively blocking IκBα phosphorylation (IC50 ~ 250 nM) and thereby prevents the induction of NF-κB p65 nuclear translocation. Shown to offer cardioprotection by reducing IL-1β and MCP-1 production (IC50<1 µM) in cardiomyocytes, and ameliorate insulin resistance in KKAy mice by regulating adiponectin release.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IKK-2
Product does not compete with ATP.
Reversible: no
Target IC50: ~ 250 nM blocking IκBα phosphorylation
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kamon, J., et al. 2004. Biochem. Biophys. Res. Commun.323, 242.
Onai, Y., et al. 2004. Cardiovasc. Res.63, 51.
Tanaka, A., et al. 2004. Blood105, 2324.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51183702
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 401482-5MG
- CAS:
- 978-62-1
