401487

IKK-2 Inhibitor VIII

The IKK-2 Inhibitor VIII, also referenced under CAS 406208-42-2, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): IKK-2 Inhibitor VIII, 2-Amino-6-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-4-(4-piperidinyl)-3-pyridinecarbonitrile, ACHP
• Empirical Formula (Hill Notation): C₂₁H₂₄N₄O₂
• CAS Number: 406208-42-2
• Molecular Weight: 364.44
• MDL number: MFCD26792569
• UNSPSC Code: 12352200
• NACRES: NA.77
• 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: yellow
• solubility: DMSO: 10 mg/mL
• shipped in: wet ice
• storage temp.: −20°C
• SMILES string: N1CCC(CC1)c2c(c(nc(c2)c3c(cccc3O)OCC4CC4)N)C#N
• InChI: 1S/C21H24N4O2/c22-11-16-15(14-6-8-24-9-7-14)10-17(25-21(16)23)20-18(26)2-1-3-19(20)27-12-13-4-5-13/h1-3,10,13-14,24,26H,4-9,12H2,(H2,23,25)
• InChI key: DYVFBWXIOCLHPP-UHFFFAOYSA-N

Description

General description

A cell-permeable piperidinyl-pyridine compound that acts as a selective inhibitor of IKK-2 activity (IC₅₀ = 8.5 and 250 nM for IKK-2 and IKK-1, respectively) with little effect towards IKK-3, Syk, and MKK4 (IC₅₀ >20 µM). Exhibits good aqueous solubility (0.12 mg/ml in pH 7.4 isotonic buffer) and potent activity in various cellular assays in vitro (IC₅₀<150 nM). Shown to be orally bioavailable both in rats and mice (BA = 60% and 16%, respectively) and effectively inhibit arachidonic acid-induced swelling in a murine ear edema model in vivo.

Biochem/physiol Actions

Target IC₅₀: 8.5 and 250 nM for IKK-2 and IKK-1, respectively

Cell permeable: yes

Primary Target
IKK-2

Product does not compete with ATP.

Reversible: no

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.

Sonication is required for complete solubilization.

Other Notes

Murata, T., et al. 2004. Bioorg. Med. Chem. Lett.14, 4019.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Irritant (B)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable