IRAK-1-4 Inhibitor I
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IRAK-1-4 Inhibitor I是IRAK-1和IRAK-4的抑制剂，IC50值分别为0.3 μM和0.2 μM[1]。
IL-1受体相关激酶在信号转导中起重要作用。IRAKs一共有4个成员，分别为IRAK-1、IRAK-2、IRAK-M和IRAK-4。IRAK-4可以激活NF-κB和MAPK途径，IRAK-4的抑制可用于抗炎治疗。IRAK-1-4 Inhibitor I是初始IRAK-4抑制剂命中的类似物，初始IRAK-4抑制剂是从抑制IRAK-4的小分子库中筛选到的。IRAK-1-4 Inhibitor I具有碱性较弱的N- ethylenemorpholine部分，比其它类似物具有更高的效力。此外，在HeLa细胞72小时增殖实验中，IRAK-1-4 Inhibitor I不具有任何细胞毒性（ED50 >30μM）[1]。
参考文献：
[1] Jay P. Powers, Shyun Li, Juan C. Jaen, Jinqian Liu, Nigel P. C. Walker, Zhulun Wang and Holger Wesche. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorganic & Medicinal Chemistry Letters. 2006, 16: 2842–2845.
- 1. Pan B, Gao J, et al. "Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice." Int Immunopharmacol. 2020;85:106597. PMID:32422509
- 2. Zha C, Zhang W, et al. "Anti-β(2)GPI/β(2)GPI induces neutrophil extracellular traps formation to promote thrombogenesis via the TLR4/MyD88/MAPKs axis activation." Neuropharmacology. 2018 Jun 5;138:140-150. PMID:29883691
- 3. Ghorpade DS, Ozcan L, et al. "Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance." Nature. 2018 Mar 29;555(7698):673-677. PMID:29562231
- 4. Chang MC, Chan CP, et al. "Areca nut components stimulate ADAM17, IL-1α, PGE2 and 8-isoprostane production in oral keratinocyte: role of reactive oxygen species,EGF and JAK signaling." Oncotarget. 2016 Mar 29;7(13):16879-94. PMID:26919242
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 395.41 |
| Cas No. | 509093-47-4 |
| Formula | C20H21N5O4 |
| Synonyms | IRAK-1/4 Inhibitor I |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥19.75 mg/mL in DMSO |
| Chemical Name | N-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide |
| SDF | Download SDF |
| Canonical SMILES | C1COCCN1CCN2C3=CC=CC=C3N=C2NC(=O)C4=CC(=CC=C4)[N+](=O)[O-] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
HeLa细胞 |
|
制备方法 |
溶于DMSO。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
72小时 |
|
实验结果 |
在一项72小时的增殖测定中，IRAK-1-4 Inhibitor I对HeLa细胞没有显示出任何的细胞毒性 (ED50 > 30 μM)。此外，IRAK-1-4 Inhibitor I显著抑制IRAK-1和IRAK-4（其IC50值分别为0.3 μM和0.2 μM）。 |
|
References: [1]. Jay P. Powers, Shyun Li, Juan C. Jaen, Jinqian Liu, Nigel P. C. Walker, Zhulun Wang and Holger Wesche. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorganic & Medicinal Chemistry Letters. 2006, 16: 2842–2845. |
|
| 描述 | IRAK-1-4 Inhibitor I是白细胞介素-1受体相关激酶（IRAK）的抑制剂，作用于IRAK-1和IRAK-4，IC50值分别为0.3 μM和0.2 μM。 | |||||
| 靶点 | IRAK-1 | IRAK-4 | ||||
| IC50 | 0.3 μM | 0.2 μM | ||||
质量控制和MSDS
- 批次:
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