SP 100030

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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)
Datasheet
Citations (2)
Reviews
Pathways (1)

Biological Activity for SP 100030

SP 100030 is a 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 for SP 100030

SP 100030 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for SP 100030

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SP 100030

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

Preparing Stock Solutions for SP 100030

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.

Select a batch to recalculate based on the batch molecular weight:
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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References for SP 100030

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


If you know of a relevant reference for SP 100030, please let us know.

View Related Products by Product Action

View all NF-κB and IκB Inhibitors

Keywords: SP 100030, 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, 5309, Tocris Bioscience

2 Citations for SP 100030

Citations are publications that use Tocris products. Selected citations for SP 100030 include:

David et al (2022) Tumor-Derived Lysophosphatidic Acid Blunts Protective Type I Interferon Responses in Ovarian Cancer. Cancer Discov 12 1904-1921 PMID: 35552618

Stephen et al (2020) TAK1 inhibition in mouse astrocyte cultures ameliorates cytokine-induced chemokine production and neutrophil migration. J Neurochem 152 697-709 PMID: 31782806


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Pathways for SP 100030

NF-κB Signaling Pathway

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.