401480

IKK Inhibitor III, BMS-345541

IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ = ~ 300 nM).

• Sinónimos: IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
• Fórmula empírica (notación de Hill): C₁₄H₁₇N₅ · 2C₂HF₃O₂
• Número de CAS: 445430-58-0
• Peso molecular: 483.36
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥96% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated (hygroscopic); protect from light
• color: off-white
• solubilidad: DMSO: 5 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C14H17N5/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15/h3-4,7-8H,5-6,15H2,1-2H3,(H,16,18)
• Clave InChI: PSPFQEBFYXJZEV-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC₅₀ = ~ 4 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC₅₀ = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC₅₀ = 1-5 µM in THP-1 cells) and in vivo (IC₅₀ = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.

A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC₅₀ ~4.0 µM) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC₅₀ = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC₅₀ = 1-5 µM in THP-1 cells) and in vivo (IC₅₀ = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~300 nM against IKK-2; 4 µM against cellular IκBα phosphorylation in THP-1 cells; 1-5 µM LPS-induced cytokine production in THP-1 cells

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Forma física

Supplied as bis-TFA salt.

Otras notas

Townsend, R.M., et al. 2004. Transplantation77, 1090.
MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508.
McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652.
Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.

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 1
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable