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Submit ReviewIKK 16
说明： Selective inhibitor of IKK
化学名： N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide hydrochloride
纯度： ≥98% (HPLC)
生物活性 for IKK 16
IKK 16 is a selective inhibitor of IκB kinase (IKK) (IC50 values are 40, 70 and 200 nM for IKKβ, IKK complex and IKKα respectively). Inhibits TNF-α-stimulated IκB degradation and expression of adhesion molecules E-selectin, ICAM and VCAM (IC50 values are 1.0, 0.5, 0.3 and 0.3 μM respectively). Inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis.
化合物库 for IKK 16
IKK 16 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for IKK 16
| 分子量 | 520.09 |
| 公式 | C28H29N5OS.HCl |
| 储存 | Desiccate at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1186195-62-9 |
| PubChem ID | 56972179 |
| InChI Key | XFVDIVQCZWDBCW-UHFFFAOYSA-N |
| Smiles | Cl.O=C(N1CCC(CC1)N1CCCC1)C1=CC=C(NC2=NC=CC(=N2)C2=CC3=CC=CC=C3S2)C=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.
溶解性数据 for IKK 16
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 26 | 50 | |
| DMSO | 26 | 50 |
制备储备液 for IKK 16
以下数据基于产品分子量 520.09。 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 |
|---|---|---|---|
| 0.5 mM | 3.85 mL | 19.23 mL | 38.45 mL |
| 2.5 mM | 0.77 mL | 3.85 mL | 7.69 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.85 mL |
| 25 mM | 0.08 mL | 0.38 mL | 0.77 mL |
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产品说明书 for IKK 16
参考文献 for IKK 16
参考文献是支持产品生物活性的出版物。
Waelchli et al (2006) Design and preparation of 2-benzoamido-pyrimidines as inhibitors of IKK. Bioorg.Med.Chem.Lett. 16 108 PMID: 16236504
If you know of a relevant reference for IKK 16, please let us know.
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关键词: IKK 16, IKK 16 supplier, Selective, inhibitors, inhibits, IKK, IκB, IkappaB, Kinases, NF-κB, NF-kappaB, NF-kB, Transcription, Factors, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, IKK16, IkB, Kinase, NF-kB/IkB, 2539, Tocris Bioscience
8 篇 IKK 16 的引用文献
引用文献是使用了 Tocris 产品的出版物。 IKK 16 的部分引用包括：
Jones et al (2017) Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation. Nat Chem Biol 13 38 PMID: 27820799
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
Shen et al (2013) Small-molecule inducer of β cell proliferation identified by high-throughput screening. J.Am.Chem.Soc. 135 1669 PMID: 23330637
Ansbro et al (2013) Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference. PLoS One 8 e60334 PMID: 23593196
Rycaj et al (2016) Longitudinal tracking of subpopulation dynamics and molecular changes during LNCaP cell castration and identification of inhibitors that could target the PSA-/lo castration-resistant cells. Oncotarget 7 14220 PMID: 26871947
Sordi et al (2015) Inhibition of IκB Kinase Attenuates the Organ Injury and Dysfunction Associated with Hemorrhagic Shock. J Neuroimmunol 21 563 PMID: 26101953
Thein et al (2014) IKK regulates the deubiquitinase CYLD at the postsynaptic density. Biochem Biophys Res Commun 450 550 PMID: 24928390
Brosnahan et al (2013) NE potentiates proinflammatory responses of human vaginal epithelial cells. Bioorg Med Chem Lett 259 42583 PMID: 23571017
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IKK 16 的评论
平均评分: 5 (Based on 1 Review.)
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IKK 16 blocks LPA-mediated COX-2 expression.
By
Anonymous on 12/13/2018
分析类型： In Vitro
种属： Human
细胞系/组织： Osteosarcoma
Human osteosarcoma cells were incubated with 5 μM IKK 16 for 30 min prior to treatment with 10 μM LPA to estimate COX-2 expression using Western blot analysis. IKK 16 abolished LPA-induced COX-2 expression
