IRAK inhibitor 6

An IRAK4 inhibitor

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库存: 现货

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数量
5mg

￥1862.00

1490.00

- +
10mg

￥2675.00

2140.00

- +
50mg

￥7000.00

5600.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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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.