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Tocris/SP 100030/5309/50/50 mg

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货号: 5309/50

品牌: Tocris

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Description: NF-κB and AP-1 dual inhibitor

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

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

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.

Compound Libraries

SP 100030 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	437.65
Formula	C₁₄H₅ClF₉N₃O
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	154563-54-9
PubChem ID	9910975
InChI Key	GHMKQBWHPQMXSH-UHFFFAOYSA-N
Smiles	O=C(NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C1=C(C(F)(F)F)N=C(Cl)N=C1

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.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	43.76	100
	ethanol	43.76	100

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 solvent 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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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

Keywords: SP 100030, supplier, SP100030, potent, dual, inhibitors, inhibits, nf-kb, nf-kappab, nf-κb, blocks, cytokine, production, selective, t, cells, immunosuppressive, anti-inflammatory, NF-kB/IkB, AP-1, NF-kB/IkB, Tocris Bioscience

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