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).

• Synonim(y): IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
• Wzór empiryczny (zapis Hilla): C₁₄H₁₇N₅ · 2C₂HF₃O₂
• Numer CAS: 445430-58-0
• Masa cząsteczkowa: 483.36
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥96% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: off-white
• rozpuszczalność: DMSO: 5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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)
• Klucz InChI: PSPFQEBFYXJZEV-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Postać fizyczna

Supplied as bis-TFA salt.

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable