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- 2026年05月27日
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- 详细信息
- 文献和实验
- 技术资料
- 英文名：
5-(2-((4-Morpholinophenyl)amino)pyrimidin-4-yl)-2-((tetrahydro-2H-pyran-4-yl)oxy)benzonitrile
- 供应商：
上海安毕达生物科技有限公司
- CAS号：
1292310-49-6
- 规格：
50μL/1mL/1mg/2mg/5mg/10mg/25mg/50mg
| 规格： | 50μL | 产品价格： | ￥239.0 |
|---|---|---|---|
| 规格： | 1mL | 产品价格： | ￥1585.0 |
| 规格： | 1mg | 产品价格： | ￥572.0 |
| 规格： | 2mg | 产品价格： | ￥1134.0 |
| 规格： | 5mg | 产品价格： | ￥1575.0 |
| 规格： | 10mg | 产品价格： | ￥2457.0 |
| 规格： | 25mg | 产品价格： | ￥3906.0 |
| 规格： | 50mg | 产品价格： | ￥5292.0 |
TANK-binding kinase 1 (TBK1) is a Ser/Thr kinase with a central role in coordinating the cellular response to invading pathogens and regulating key inflammatory signaling cascades. While intact TBK1 signaling is required for successful anti-viral signaling, dysregulated TBK1 signaling has been linked to a variety of pathophysiologic conditions, including cancer2.TANK-binding kinase 1 (TBK1) plays pivotal roles in antiviral innate immunity. TBK1 mediates the activation of interferon regulatory factor (IRF) 3, leading to the induction of type I IFNs (IFN-α/β) following viral infections. TBK1 must be tightly regulated to effectively control viral infections and maintain immune homeostasis. TBK1 activity can be regulated in a variety of ways, such as phosphorylation, ubiquitination, kinase activity modulation and prevention of functional TBK1-containing complexes formation3.Reducing the activity or expression of TBK1 led to reduction in α-smooth muscle actin stress fiber levels by 40-60% and deposition of ECM components collagen I and fibronectin by 50% in TGF-β-stimulated normal and IPF fibroblasts. YAP and TAZ are homologous mechanoregulatory profibrotic transcription cofactors known to regulate fibroblast activation. TBK1 knockdown or inhibition decreased the total and nuclear protein levels of YAP/TAZ4.TBK1 directly phosphorylates RAB7AS72, but not several other RABs known to be phosphorylated on the homologous residue by LRRK2, in vitro, and this modification requires PARKIN activity in vivo5.TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor. TBK1/IKKε-IN-2 (Cmpound #1) inhibits TBK1 biochemical function in Ulight kinase assay at 5 and 250 μM ATP concentration with IC50s of 0.6 and 2.6 nM, rsespectively. TBK1/IKKε-IN-2 inhibits IKKε biochemical function in Ulight kinase assay at 10 μM ATP with an IC50 of 3.9 nM. The IC50 of TBK1/IKKε-IN-2 in the Panc 02.13 proliferation assay is 5 μM6.
溶解方案(细胞实验)
DMSO 中的溶解度 : 21.5 mg/mL (46.99 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)
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文献和实验Or-Yam Revach,et al. Targeting TANK-binding kinase 1 (TBK1) in cancer. Expert Opin Ther Targets. 2020 Nov;24(11):1065-1078.
Wei Zhao,et al. Negative regulation of TBK1-mediated antiviral immunity. FEBS Lett.2013 Mar 18;587(6):542-8.
Aja Aravamudhan,et al. TBK1 regulates YAP/TAZ and fibrogenic fibroblast activation. Am J Physiol Lung Cell Mol Physiol. 2020 May 1;318(5):L852-L863.
J-M Heo,et al. RAB7A phosphorylation by TBK1 promotes mitophagy via the PINK-PARKIN pathway. Sci Adv. 2018 Nov 21;4(11):eaav0443.
Muvaffak A, et al. Evaluating TBK1 as a therapeutic target in cancers with activated IRF3. Mol Cancer Res. 2014 Jul;12(7):1055-66.
Sci Signal 封面文章：赵振东 / 王健伟等揭示转录因子 ID2 抑制抗病毒天然免疫机制
天然免疫是机体抗病毒感染的第一道防线。机体为清除侵入的病毒必须启动有效的天然免疫应答，为避免过度天然免疫反应导致免疫病理损伤和清除入侵的病毒后快速恢复细胞内环境稳态，宿主细胞进化出多样的机制以调控天然免疫应答的强度。 2022 年 1 月 4 日，中国医学科学院病原生物学研究所赵振东课题组和王健伟课题组在 Science Signaling 期刊发表题为：ID2 inhibits innate antiviral immunity by blocking TBK1- and IKKε
,2F12;CRIS-3 Leu LFA-1(gp180/95)的α链 与ICAM-1（CD54）和ICAM-2（CD102）结合 CD11b Mol,OKM1; (Mac-1,CR3,integrin αm G,M,NK gp165/95的α链 C3bi和FB受体，与ICAM-1结合，粘附，调理吞噬 CD11c LeuM5;(CR4,integrin αx) M,G,NK,Tsub gp150/95的α链 C3bi受体，调理吞噬
TRAF‐Mediated TNFR‐Family Signaling
TRAF2, TANK and TBK1, a novel IKK‐related kinase. Embo J. 18:6694‐6704. Pullen, S.S., Miller, H.G., Everdeen, D.S., Dang, T.T., Crute, J.J., and Kehry, M.R. 1998. CD40‐tumor
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