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Potent dual inhibitor of NF-κB and AP-1 transcriptional activity (IC50 = 50 nM). Blocks production of IL-2, IL-8 and TNF-α from Jurkat T cells. Inhibits cytokine production selectively in T cells; exhibits minimal inhibition of cytokine production in other cell types. Decreases arthritic severity in a mouse model of collagen-induced arthritis. Also ameliorates muscle wasting in a rat model of cancer cachexia.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 437.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.28 mL||11.42 mL||22.85 mL|
|5 mM||0.46 mL||2.28 mL||4.57 mL|
|10 mM||0.23 mL||1.14 mL||2.28 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the biological activity of the product.
Gerlag et al (2000) The effect of a T cell-specific NF-κB inhibitor on in vitro cytokine production and collagen-induced arthritis J.Immunol. 165 1652 PMID: 10903776
Sullivan et al (1998) 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-κB- and AP-1-mediated gene expression identified using solution-phase combinatorial ch J.Med.Chem. 41 413 PMID: 9484492
Moore-Carrasco et al (2007) The AP-1/NF-κB double inhibitor SP100030 can revert muscle wasting during experimental cancer cachexia. Int.J.Oncol. 30 1239 PMID: 17390027
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