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IRAK inhibitor 1
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 1图片
CAS NO:1042224-63-4
包装与价格:
包装价格(元)
10mg电议
5mg电议
50mg电议
500mg电议
1g电议

产品介绍
IRAK inhibitor 1 是一种有效的 IRAK-4 抑制剂,IC50 为 216 nM,对 JNK-1 和 JNK-2 活性较差,IC50 分别为 3.801 μM 和 >10 μM。
Cas No.1042224-63-4
别名环巴胺抑制剂1
化学名6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine
Canonical SMILESC1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4
分子式C17H19N5
分子量293.37
溶解度Soluble 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: 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.