401482

IKK-2 Inhibitor V

The IKK-2 Inhibitor V, also referenced under CAS 978-62-1, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): IKK-2 Inhibitor V, N-(3,5-Bis-trifluoromethylphenyl)-5-chloro-2-hydroxybenzamide, IMD-0354
• Empirical Formula (Hill Notation): C₁₅H₈ClF₆NO₂
• CAS Number: 978-62-1
• Molecular Weight: 383.67
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00218820
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: ethanol: 1 mg/mL, DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: FC(F)(F)c1cc(cc(c1)C(F)(F)F)NC(=O)c2c(ccc(c2)Cl)O
• InChI: 1S/C15H8ClF6NO2/c16-9-1-2-12(24)11(6-9)13(25)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6,24H,(H,23,25)
• InChI key: CHILCFMQWMQVAL-UHFFFAOYSA-N

Description

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 KKA_y 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 KKA_y 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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3