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SC 514

Cat. No. 3318 3 篇引用文献 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Discontinued Product

3318 has been discontinued.

说明： IKKβ inhibitor; attenuates NF-κB-induced gene expression
化学名： 4-Amino-[2',3'-bithiophene]-5-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献 (3)
评论 (1)
生物活性 技术数据 说明书 参考文献

生物活性 for SC 514

SC 514 is an orally active, ATP-competitive IKKβ inhibitor (IC50 = 3 - 12 μM) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50 values are 20, 20 and 8 μM respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo.

许可信息

Sold for research purposes under agreement from AstraZeneca

技术数据 for SC 514

分子量 224.3
公式 C9H8N2OS2
储存 Store at +4°C
纯度 ≥98% (HPLC)
CAS Number 354812-17-2
PubChem ID 2807869
InChI Key BMUACLADCKCNKZ-UHFFFAOYSA-N
Smiles NC1=C(C(N)=O)SC(C2=CSC=C2)=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.

参考文献 for SC 514

参考文献是支持产品生物活性的出版物。

Kishore et al (2003) A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts. J.Biol.Chem. 278 32861 PMID: 12813046

Gomez et al (2005) Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br.J.Pharmacol. 146 217 PMID: 15997236

Baxter et al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 14 2817

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关键词: SC 514, SC 514 supplier, IKK-2, inhibitors, inhibits, attenuates, NF-κB, NF-kappaB-induced, gene, expression, NF-kB, IKK, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, NF-kappaB, Cytokine, Signaling, Signalling, Transcription, Factors, SC514, AstraZeneca, NF-kB/IkB, IkB, Kinase, 3318, Tocris Bioscience

3 篇 SC 514 的引用文献

引用文献是使用了 Tocris 产品的出版物。 SC 514 的部分引用包括：

Akhtar et al (2015) MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes. Nature 67 423 PMID: 25385442

Gurney et al (2019) Inhibition of Inflammatory Changes in Human Myometrial Cells by Cell Penetrating Peptide and Small Molecule Inhibitors of NFκB. Front Immunol 9 2966 PMID: 30619324

Cataldi et al (2015) Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1. Virology 485 340 PMID: 26331681

SC 514 的评论

平均评分: 5 (Based on 1 Review.)

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SC 514 inhibits LPS-mediated inflammation.
By Anonymous on 12/11/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： Macrophages

RAW macrophages were incubated with 1 mM SC 514 for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with SC 514.

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