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CAS No.: 1292310-49-6

TBK1/IKKε-IN-2 Catalog No. CSN16345

Synonyms: Ikk epsilon-in-1;IKKε-IN-1;MDK10496

IKKε-IN-1 is a potent IKKε inhibitor. It inhibits the in-situ ΙKΚ ε-mediated phosphorylation of IRF3 with an IC50 value of less than about 100 nM.

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技术信息

生物活性

描述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 cancer^[2].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 formation^[3].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/TAZ^[4].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 vivo^[5].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 μM^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1857 mL
- 10.9284 mL
- 21.8568 mL
- 5 mM
- 0.4371 mL
- 2.1857 mL
- 4.3714 mL
- 10 mM
- 0.2186 mL
- 1.0928 mL
- 2.1857 mL

技术信息

CAS号

1292310-49-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H27N5O3

运输

蓝冰

分子量

457.52

别名

Ikk epsilon-in-1;IKKε-IN-1;MDK10496

溶解度

DMSO	60.0 mg/mL (131.1 mM)
Water	Insoluble
Ethanol	Insoluble

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TBK1/IKKε-IN-2 Catalog No. CSN16345

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