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
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About This Item
Wzór empiryczny (zapis Hilla):
C14H17N5 · 2C2HF3O2
Numer CAS:
Masa cząsteczkowa:
483.36
Kod UNSPSC:
12352200
NACRES:
NA.77
Polecane produkty
Poziom jakości
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 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.
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
Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 1
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
Certyfikaty analizy (CoA)
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