TBK1-IKKε inhibitor II

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TBK1-IKKε抑制剂 II 是一种有效的、选择性的 TBK1/IKKε 双重抑制剂，IC50 分别为 13 nM/59 nM。

TBK1-IKKε inhibitor II is a potent, selective dual inhibitor of TBK1/IKKε with IC50 of 13 nM/59 nM, respectively; displays 100- to 1000-fold less activity against other tested protein kinases including PDK1, PI3K family members and mTOR; inhibits LPS-induced expression of IFNβ (IC50=62 nM), and the IFNβ target genes IP10 (IC50=78 nM) and Mx1 (IC50=20 nM); effectively blocks TLR3-dependent IRF3 nuclear translocation in cells with IC50<100 nM.

TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells).TBK1/IKKε-IN-4 (Compound II; 0-2 μM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity.TBK1/IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC50 =62 nM), and the IFNβ target genes IP10 (IC50 =78 nM) and Mx1 (IC50=20 nM). TBK1/IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 μM. Western Blot Analysis Cell Line:HCC44 cells Concentration:0 μM, 0.5 μM, 1 μM, 2 μM Incubation Time:30 minutes Result:Was sufficient to blunt baseline AKT activity.

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Immunology/Inflammation

IκB kinase (IKK)

IκB kinase (IKK)

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1381930-17-1

533.633

C28H35N7O4

>98% (HPLC)

In Vitro:?DMSO : 70 mg/mL (131.18 mM)

CN1CCN(CC1)CCCOC2=CC(=CC(=C2OC)OC)NC3=NC=C4C=NN(C4=N3)C5=CC=C(C=C5)OC

N-(3,4-dimethoxy-5-(3-(4-methylpiperazin-1-yl)propoxy)phenyl)-1-(4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine

(-20℃)

With Ice Pack

≥ 2 years