TBK1/IKKε-IN-4 |
| Katalog-Nr.GC63212 |
TBK1/IKKε -IN-4 ist ein 6-Aminopyrazolopyrimidin-Derivat und ein wirksames, selektives TBK1 und IKKε Inhibitor mit IC50-Werten von 13 nM bzw. 59 nM. TBK1/IKKε-IN-4 zeigt eine 100- bis 1000-fach geringere AktivitÄt gegen andere Proteinkinasen, einschließlich PDK1, Mitglieder der PI3K-Familie und mTOR.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1381930-17-1
Sample solution is provided at 25 µL, 10mM.
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TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1].
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)[1].TBK1/IKKε-IN-4 (Compound II; 0-2 µM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity[1].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[1].
[1]. Ou YH, et al. TBK1 directly engages Akt/PKB survival signaling to support oncogenic transformation. Mol Cell. 2011 Feb 18;41(4):458-70.
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