SP 100030

Pricing Availability Delivery Time Qty
Cat.No. 5309 - SP 100030 | C14H5ClF9N3O | CAS No. 154563-54-9
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)
Datasheet
Citations
Reviews
Literature
Pathways

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

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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

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Product Datasheets

Safety Datasheet

References

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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View all NF-κB and IκB Inhibitors

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Citations for SP 100030

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Literature in this Area

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Asthma

Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

Pathways for SP 100030

NF-κB

NF-κB Signaling Pathway

NF-κB signaling plays an important role in inflammation, the innate and adaptive immune response and stress. Dysregulated signaling can occur in inflammatory and autoimmune diseases.