CAS NO: | 1042672-97-8 |
规格: | 98% |
分子量: | 396.46 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
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.