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IRAK inhibitor 6
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 inhibitor 6图片
CAS NO:1042672-97-8
规格:98%
分子量:396.46
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
IRAK-4 inhibitor
CAS:1042672-97-8
分子式:C20H20N4O3S
分子量:396.46
纯度:98%
存储:Store at -20°C

Background:

IC50: 0.16 μM for IRAK-4


IRAK inhibitor 6 is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor.


The interleukin-1 receptor associated kinases (IRAKs) are a family of serine/threonine kinases related with regulating cellular signalling downstream of the IL-18, IL-1 and various Toll-like receptors. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NFКB and MAPK pathways, which are critical for the production of inflammatory cytokines.


In vitro: A quantitative structure–activity relationship (QSAR) study of IRAK inhibitor 6 and its analogs were conducted by using the genetic algorithm and multiple linear regression (GA-MLR) method [1]. In vitro study showed that compared with its unsubstituted phenyl amide analog, the ortho-substitution with chloro, methoxy and difluoromethoxy analogs of IRAK inhibitor 6 improved potency against IRAK-4 significantly. These potency effects were additive, with the most active example in the set being IRAK inhibitor 6, in which the presence of nitrogen-linked substituents at the para position had a beneficial effect on the rate of turnover by human microsomes (20 μL/min/mg protein) [2].


Clinical trial: N/A


参考文献:
[1] Pourbasheer E,?Riahi S,?Ganjali MR,?Norouzi P.  Quantitative structure-activity relationship (QSAR) study of interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor activity by the genetic algorithm and multiple linear regression (GA-MLR) method. J Enzyme Inhib Med Chem.?2010 Dec;25(6):844-53.
[2] Buckley GM,?Gowers L,?Higueruelo AP,?Jenkins K,?Mack SR,?Morgan T,?Parry DM,?Pitt WR,?Rausch O,?Richard MD,?Sabin V,?Fraser JL.  IRAK-4 inhibitors. Part 1: a series of amides. Bioorg Med Chem Lett.?2008 Jun 1;18(11):3211-4.