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Submit ReviewIMD 0354
说明： Inhibitor of IKKβ; also exhibits antibacterial activity
化学名： N-[3,5-Bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide
纯度： ≥99% (HPLC)
生物活性 for IMD 0354
IMD 0354 is an inhibitor of IκB kinase-β (IKKβ) that blocks NF-κB nuclear translocation. Attenuates myocardial ischemia/reperfusion injury by decreasing expression of adhesion molecules ICAM-1 and P-selectin and inhibiting cytokine and chemokine production in cardiomyocytes. Induces G0/G1 cell cycle arrest and apoptosis in HMC-1 and breast cancer cells. Antagonist at P2X1, P2X4 and P2X7 receptors (IC50 values are 19, 156 and 175 nM respectively). Inhibits platelet aggregation induced by collagen in vitro. Exhibits potent antibacterial activity against MRSA in C. elegans model (MIC = 0.06 μg/mL). Selective aquaporin 4 inhibitor (IC50 values are 210 nM, 390 nM and 420 nM at rat, mouse and human receptors, respectively).
技术数据 for IMD 0354
| 分子量 | 383.67 |
| 公式 | C15H8ClF6NO2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 978-62-1 |
| PubChem ID | 5081913 |
| InChI Key | CHILCFMQWMQVAL-UHFFFAOYSA-N |
| Smiles | OC1=C(C=C(Cl)C=C1)C(=O)NC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F |
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 IMD 0354
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 38.36 | 100 | |
| ethanol | 38.36 | 100 |
制备储备液 for IMD 0354
以下数据基于产品分子量 383.67。 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 | 2.61 mL | 13.03 mL | 26.06 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.21 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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产品说明书 for IMD 0354
参考文献 for IMD 0354
参考文献是支持产品生物活性的出版物。
Onai et al (2004) Inhibition of IκB phosphorylation in cardiomyocytes attenuates myocardial ischemia/reperfusion injury. Cardiovasc.Res. 63 51 PMID: 15194461
Tanaka et al (2006) A new IκB kinase β inhibitor prevents human breast cancer progression through negative regulation of cell cycle transition. Cancer Res. 66 419 PMID: 16397257
Tanaka et al (2005) A novel NF-κB inhibitor, IMD-0354, supresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors. Hematopoiesis 105 2324
Escobar et al (2020) New antimicrobial bioactivity against multidrug resistant gram-positive bacteria of kinase inhibitor IMD0354. Antibiotics 9 665 PMID: 33019726
If you know of a relevant reference for IMD 0354, please let us know.
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关键词: IMD 0354, IMD 0354 supplier, inhibitors, inhibits, IKK-2, IKK, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, NF-κB, NF-kappaB, NF-kB, Cytokine, Signaling, Signalling, Transcription, Factors, IMD0354, AER270, IkB, Kinase, NF-kB/IkB, P2X, Receptors, Antibiotics, Aquaporins, 2611, Tocris Bioscience
6 篇 IMD 0354 的引用文献
引用文献是使用了 Tocris 产品的出版物。 IMD 0354 的部分引用包括：
Zhang et al (2018) Tumor-Stroma IL1β-IRAK4 Feedforward Circuitry Drives Tumor Fibrosis, Chemoresistance, and Poor Prognosis in Pancreatic Cancer. Cancer Res 78 1700 PMID: 29363544
Chen et al (2015) Pentoxifylline Attenuates Proteinuria in Anti-Thy1 Glomerulonephritis via Downregulation of Nuclear Factor-κB and Smad2/3 Signaling. J Mol Neurosci 21 276 PMID: 25879629
Escobar et al (2020) New antimicrobial bioactivity against multidrug resistant gram-positive bacteria of kinase inhibitor IMD0354. Antibiotics 9 665 PMID: 33019726
Zwicker et al (2015) Interleukin 34: a new modulator of human and experimental inflammatory bowel disease. Clin Sci (Lond) 129 281 PMID: 25896238
Kong et al (2015) Tumor-suppressive microRNA-497 targets IKKβ to regulate NF-κB signaling pathway in human prostate cancer cells. Am J Cancer Res 5 1795 PMID: 26175947
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
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IMD 0354 的评论
平均评分: 5 (Based on 1 Review.)
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IMD 0354 ameliorates LPS-induced TNFa production.
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 5 μM IMD 0354 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 IMD 0354.
