IRAK inhibitor 1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
对IRAK-4的IC50值为35 nM。
白介素-1受体相关激酶(IRAK)由四个家族成员组成:IRAK-1、IRAK-2、IRAK-3/M和IRAK-4。一经其上游同源受体活化,IRAK-4磷酸化IRAK1,引起IRAK-1的活化和自磷酸化以及随后下游底物的磷酸化。IRAK抑制剂1是白介素-1受体相关激酶4 (IRAK-4)的抑制剂。
体内试验:区域异构吡啶IRAK抑制剂1(6)和其类似物(7)表现出对比鲜明的SAR,2,6-吡啶异构体IRAK抑制剂1具有低纳摩尔效能,而2,4-吡啶异构体7则表现出较小的活性,尽管其含有一个更易结合的双配位基结合基序。10 μM IRAK抑制剂1能抑制39%的JNK-1和15%的JNK-2[1]。
体内试验:目前无IRAK抑制剂1及其类似物的动物实验。
临床试验:IRAK抑制剂1目前正处于临床前开发阶段,无法获得临床数据。
参考文献:
[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.
- 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
Storage | Store at -20°C |
M.Wt | 293.37 |
Cas No. | 1042224-63-4 |
Formula | C17H19N5 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥14.4 mg/mL in DMSO |
Chemical Name | 6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine |
SDF | Download SDF |
Canonical SMILES | C1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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 |
质量控制和MSDS
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