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Submit ReviewSP 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.
SP 100030 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 437.65 |
公式 | C14H5ClF9N3O |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 43.76 | 100 | |
ethanol | 43.76 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 SP 100030 的部分引用包括:
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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