SP 100030

Cat. No. 5309

SP 100030 C14H5ClF9N3O [154563-54-9]

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Chemical Name: N-[3,5-Bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)-5-pyrimidinecarboxamide

Biological Activity

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.

Technical Data

M.Wt:
437.65
Formula:
C14H5ClF9N3O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
154563-54-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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 chemistry. J.Med.Chem. 41 413. PMID: 9484492.

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Keywords: SP 100030, supplier, SP100030, potent, dual, inhibitors, inhibits, nf-kb, nf-kappab, nf-κb, blocks, cytokine, production, selective, t, cells, immunosuppressive, anti-inflammatory, Tocris Bioscience, NF-κB and IκB Inhibitor products

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