407602
Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor
InSolution, ≥98%
别名:
InSolution Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor, N-(1-(2-morpholinoethyl)-1H-benzo[d]imidazol-2-yl)-3-nitrobenzamide, N-(2-Morpholinylethyl)-2-(3-nitrobenzoylamido)-benzimidazole
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About This Item
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质量水平
方案
≥98% (HPLC)
表单
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light
运输
dry ice
储存温度
−70°C
SMILES字符串
[N+](=O)([O-])c1cc(ccc1)C(=O)Nc2[n](c4c(n2)cccc4)CCN3CCOCC3
InChI
1S/C20H21N5O4/c26-19(15-4-3-5-16(14-15)25(27)28)22-20-21-17-6-1-2-7-18(17)24(20)9-8-23-10-12-29-13-11-23/h1-7,14H,8-13H2,(H,21,22,26)
InChI key
QTCFYQHZJIIHBS-UHFFFAOYSA-N
一般描述
A cell-permeable benzimidazole compound that acts as a potent and selective inhibitor of interleukin-1 receptor-associated kinases (IC50 = 300 nM and 200 nM for IRAK-1 and -4). Shown to exhibit little activity against a panel of 27 other kinases (IC50 >10 µM), including lck and src. The solid form of this compound (Cat. No. 407601) is also available.
生化/生理作用
Primary Target
IRAK-1/4
IRAK-1/4
Reversible: yes
Target IC50: 300 nM and 200 nM for IRAK-1 and -4
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
外形
A 25 mM (5 mg/506 µL) solution of Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor (Cat. No. 407601) in DMSO.
重悬
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
其他说明
Srivastava, R., et al. 2012. Cancer Res.72, In press.
Bhattacharyya, S., et al. 2007. Am. J. Physiol. Gastrointest. Liver Physiol.293, G429.
Powers, J.P., et al. 2006. Bioorg. Med. Chem. Lett.16, 2842.
Bhattacharyya, S., et al. 2007. Am. J. Physiol. Gastrointest. Liver Physiol.293, G429.
Powers, J.P., et al. 2006. Bioorg. Med. Chem. Lett.16, 2842.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
10 - Combustible liquids
WGK
WGK 2
闪点(°F)
188.6 °F - closed cup - (refers to pure substance)
闪点(°C)
87 °C - closed cup - (refers to pure substance)
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Combination of docetaxel, cisplatin and 5-FU, known as TPF, is an FDA-approved treatment for head and neck squamous cell carcinoma (HNSCC). Acquired chemo-resistance to TPF, a primary reason for non-responsiveness to the treatment and relapse of tumor is a major
Ratika Srivastava et al.
Cancer research, 72(23), 6209-6216 (2012-10-09)
Toll-like receptors (TLR) are expressed by a variety of cancers, including melanoma, but their functional contributions in cancer cells are uncertain. To approach this question, we evaluated the effects of stimulating or inhibiting the TLR/IL-1 receptor-associated kinases IRAK-1 and IRAK-4
Jay P Powers et al.
Bioorganic & medicinal chemistry letters, 16(11), 2842-2845 (2006-03-28)
High-throughput screening of a small-molecule compound library resulted in the identification of a novel series of N-acyl 2-aminobenzimidazoles that are potent inhibitors of interleukin-1 receptor-associated kinase-4.
Sumit Bhattacharyya et al.
American journal of physiology. Gastrointestinal and liver physiology, 293(2), G429-G437 (2007-06-02)
Lipopolysaccharide (LPS) is recognized as an inducer of the inflammatory response associated with gram-negative sepsis and systemic inflammatory response syndrome. LPS induction proceeds through Toll-like receptor (TLR) in immune cells and intestinal epithelial cells (IEC). This report presents the first
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