| Identification | Back Directory | [Name]
TBK1-IKKε inhibitor II | [CAS]
1381930-17-1 | [Synonyms]
TBK1/IKKε-IN-4
TBK1-IKKε inhibitor II
TBK1/IKKε-IN-4，TBK1-IKKε inhibitor II
1H-Pyrazolo[3,4-d]pyrimidin-6-amine, N-[3,4-dimethoxy-5-[3-(4-methyl-1-piperazinyl)propoxy]phenyl]-1-(4-methoxyphenyl)- | [Molecular Formula]
C28H35N7O4 | [MDL Number]
MFCD30186589 | [MOL File]
1381930-17-1.mol | [Molecular Weight]
533.62 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture and light | [solubility ]
DMSO : 70 mg/mL (131.18 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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]. | [IC 50]
IKKε: 59 nM (IC50); TBK1: 13 nM (IC50) | [References]
[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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