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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
IRAK inhibitor 6 是白细胞介素-1 受体相关激酶 4 (IRAK-4) 的抑制剂,IC50 为 160 nM。
Cas No.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
化学名N-(2-methoxy-4-morpholin-4-ylphenyl)-2-pyridin-3-yl-1,3-thiazole-4-carboxamide
Canonical SMILESCOC1=C(C=CC(=C1)N2CCOCC2)NC(=O)C3=CSC(=N3)C4=CN=CC=C4
分子式C20H20N4O3S
分子量396.46
溶解度≥ 9.9 mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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

References:
[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.