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).

• Sinonimo/i: IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
• Formula empirica (notazione di Hill): C₁₄H₁₇N₅ · 2C₂HF₃O₂
• Numero CAS: 445430-58-0
• Peso molecolare: 483.36
• Numero MDL: MFCD18089812
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥96% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: off-white
• Solubilità: DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: [n]21c(ncc2C)c(nc3c1cc(cc3)C)NCCN
• 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); PSPFQEBFYXJZEV-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Stato fisico

Supplied as bis-TFA salt.

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable