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  • IRAK inhibitor 6
IRAK inhibitor 6的可视化放大

IRAK inhibitor 6

An IRAK4 inhibitor

原价
¥1862-7000
价格
1490-5600
IRAK inhibitor 6的二维码

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  • 库存: 现货
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  • 货号: ajci18984
  • CAS: 1042672-97-8
  • 别名: N-[2-甲氧基-4-(4-吗啉基)苯基]-2-(3-吡啶基)-4-噻唑甲酰
  • 分子式: C20H20N4O3S
  • 分子量: 396.46
  • 纯度: >98%
  • 溶解度: ≥ 9.9 mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

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.

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