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IRAK inhibitor 1

现货
Catalog No.
A3500
IRAK-4抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,700.00
现货
10mg
¥ 3,680.00
现货
50mg
¥ 9,570.00
现货

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Background

IC50: 35 nM for IRAK-4

The interleukin-1 receptor associated kinase (IRAK) family is comprised of four family members IRAK-1, IRAK-2, IRAK-3/M, and IRAK-4. Upon activation of their upstream cognate receptors, IRAK-4 is thought to phosphorylate IRAK-1 resulting in the activation and autophosphorylation of IRAK-1 an subsequent phosphorylation of downstream substrates. IRAK inhibitor 1 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4).

In vitro: The regioisomeric pyridines IRAK inhibitor 1 (6) and it analogue (7) showed contrasting SAR, with the 2,6-pyridine isomer IRAK inhibitor 1 having low-nanomolar potency whilst the 2,4-pyridine isomer 7 showed little activity, despite having a more accessible bidentate-binding motif. At 10 μM, IRAK inhibitor 1 was found to have 39% inhibition for JNK-1 and 15% inhibition for JNK-2, respectivley [1].

In vivo: No animal in-vivo data available currently IRAK inhibitor 1 and its analogues.

Clinical trial: IRAK inhibitor 1 is currently in the preclinical development stage and no clinical data are available.

Reference:
[1] Buckley GM, Ceska TA, Fraser JL, Gowers L, Groom CR, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V.   IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008;18(11):3291-5.

文献引用

1.Upadhyay K, Park JE, et al. "Group B Streptococci Induce Proinflammatory Responses via a Protein Kinase D1-Dependent Pathway." J Immunol. 2017 Jun 1;198(11):4448-4457. PMID:28461572
2.Marinho FV, Fahel JS, et al. "Lack of IL-1 Receptor-Associated Kinase-4 Leads to Defective Th1 Cell Responses and Renders Mice Susceptible to Mycobacterial Infection." J Immunol. 2016 Sep 1;197(5):1852-63. PMID:27439514

Chemical Properties

StorageStore at -20°C
M.Wt293.37
Cas No.1042224-63-4
FormulaC17H19N5
SolubilitySoluble in DMSO
Chemical Name6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine
SDFDownload SDF
Canonical SMILESC1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Description IRAK inhibitor 1是白介素-1受体相关激酶4 (IRAK-4)的抑制剂。
靶点 IRAK-4          
IC50            

质量控制

化学结构

IRAK inhibitor 1

相关生物数据

IRAK inhibitor

相关生物数据

IRAK inhibitor