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IRAK-1-4 Inhibitor I
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IRAK-1-4 Inhibitor I图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
20mg电议
50mg电议
100mg电议

产品介绍
IRAK-1-4 Inhibitor I 是一种白介素 1 受体相关激酶 1/4 (IRAK 1/4) 的抑制剂,IC50 分别为 0.2 μM 和 0.3 μM。

Cell lines

HeLa cells

Preparation method

Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

72 hrs

Applications

In a 72-hr proliferation assay, IRAK-1-4 Inhibitor I did not show any cytotoxicity in HeLa cells (ED50 >30 μM). In addition, IRAK-1-4 Inhibitor I significantly inhibited IRAK-1 and IRAK-4 (IC50 = 0.3 μM and 0.2 μM, respectively).

产品描述

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.