1. NF-κB
  2. IKK
  3. TBK1/IKKε-IN-4

TBK1/IKKε-IN-4 

Cat. No.: HY-124652
Handling Instructions

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.

For research use only. We do not sell to patients.

TBK1/IKKε-IN-4 Chemical Structure

TBK1/IKKε-IN-4 Chemical Structure

CAS No. : 1381930-17-1

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Description

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].

IC50 & Target[1]

IKKε

59 nM (IC50)

TBK1

13 nM (IC50)

In Vitro

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].

Western Blot Analysis[1]

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.
Molecular Weight

533.62

Formula

C₂₈H₃₅N₇O₄

CAS No.

1381930-17-1

SMILES

COC1=CC=C(N2N=CC3=CN=C(NC4=CC(OCCCN5CCN(C)CC5)=C(OC)C(OC)=C4)N=C32)C=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TBK1/IKKε-IN-4IKKIκB kinaseI kappa B kinaseTBK1IKKε6-aminopyrazolopyrimidineLPSIFNβIP10IRF3AKTInhibitorinhibitorinhibit

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