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IRAK-1-4 Inhibitor I

现货
Catalog No.
A3505
IRAK-1/4抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
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10mg
¥ 1,190.00
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20mg
¥ 1,900.00
现货
50mg
¥ 4,800.00
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100mg
¥ 8,040.00
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Background

IRAK-1-4 Inhibitor I is an inhibitor of both IRAK-1 and IRAK-4 with IC50 values of 0.3μM and 0.2μM , respectively [1].

IL-1 receptor-associated kinases play important roles in signal transduction. There are totally four members of the IRAKs, they are IRAK-1, IRAK-2, IRAK-M and IRAK-4. IRAK-4 can activate NF-κB and MAPK pathways and it is shown that the inhibition of IRAK-4 can be an anti-inflammatory therapy. IRAK-1-4 Inhibitor I is an analog of an Initial IRAK-4 inhibitor hit, which is screened out from a small molecule li brary against IRAK-4. With the less basic N-ethylenemorpholine moiety, IRAK-1-4 Inhibitor I has a higher potency than other analogs. Additionally, it does not show any cytotoxicity in a 72 h proliferation assay in HeLa cells(ED50 >30μM) [1].

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.

文献引用

1. 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
2. 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
3. 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

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt395.41
Cas No.509093-47-4
FormulaC20H21N5O4
SynonymsIRAK-1/4 Inhibitor I
Solubility≥19.75 mg/mL in DMSO, <2.57 mg/mL in EtOH, <2.19 mg/mL in H2O
Chemical NameN-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide
SDFDownload SDF
Canonical SMILESC1COCCN1CCN2C3=CC=CC=C3N=C2NC(=O)C4=CC(=CC=C4)[N+](=O)[O-]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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.

生物活性

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

化学结构

IRAK-1-4 Inhibitor I

相关生物数据

IRAK-1-4 Inhibitor I

相关生物数据

IRAK-1-4 Inhibitor I

相关生物数据

IRAK-1-4 Inhibitor I