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).
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Synonym(s):
IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
Empirical Formula (Hill Notation):
C14H17N5 · 2C2HF3O2
Recommended Products
Quality Level
Assay
≥96% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
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)
InChI key
PSPFQEBFYXJZEV-UHFFFAOYSA-N
General description
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.
Biochem/physiol Actions
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
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
Supplied as bis-TFA salt.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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