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.

• Sinónimos: IKK-2 Inhibitor VIII, 2-Amino-6-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-4-(4-piperidinyl)-3-pyridinecarbonitrile, ACHP
• Fórmula empírica (notación de Hill): C₂₁H₂₄N₄O₂
• Número de CAS: 406208-42-2
• Peso molecular: 364.44
• Número MDL: MFCD26792569
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 10 mg/mL
• Condiciones de envío: wet ice
• temp. de almacenamiento: −20°C
• cadena SMILES: 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)
• Clave InChI: DYVFBWXIOCLHPP-UHFFFAOYSA-N

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
IKK-2

Product does not compete with ATP.

Reversible: no

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

Envase

Packaged under inert gas

Advertencia

Toxicity: Irritant (B)

Nota de preparación

Sonication is required for complete solubilization.

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 2
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable