BX795
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Cat.code:
tlrl-bx7
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ABOUT
TBK1/IKKε inhibitor
BX795 is a potent inhibitor of the noncanonical IkB kinases TANK-binding kinase 1 (TBK1) and IkappaB kinase-epsilon (IKKε) [1]. TBK1 and IKKε play a central role in the innate immune response. Notably, these noncanonical IkappaB kinase homologs are essential components of the interferon regulatory factor (IRF) signaling pathway.
Mode of action:
BX795 inhibits the catalytic activity of TBK1/IKKε by blocking their phosphorylation. BX795, an aminopyrimidine compound, was developed as an inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) [1].
Studies have demonstrated that BX795 is a potent inhibitor of the IKK-related kinases, TANK-binding kinase 1 (TBK1), and IKKε, and hence of IRF3 activation and IFN-β production [2, 3].
Key features:
- A potent inhibitor of TBK1 and IKK-ε
- InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested
References:
1. Feldman RL. et al., 2005. Novel Small Molecule Inhibitors of 3-Phosphoinositide- dependent Kinase-1. J. Biol. Chem., 280: 19867 - 19874.
2. Clark K. et al., 2009. Use of the Pharmacological Inhibitor BX795 to Study the Regulation and Physiological Roles of TBK1 and I{kappa}B Kinase {epsilon}: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J. Biol. Chem., 284: 14136 - 14146.
3. Bain J. et al., 2007. The selectivity of protein kinase inhibitors: a further update, 408: 297-315.
All products are for research use only, and not for human or veterinary use.
InvitroFit™
InvitroFit™ is a high-quality standard specifically adapted for in vitro studies of inhibitors. InvitroFit™ products are highly pure (≥95%) and guaranteed free of bacterial contamination, as confirmed using HEK Blue™ TLR2 and HEK Blue™ TLR4 cellular assays. Each lot is rigorously tested for functional activity using validated (or proprietary) cellular models. This grade ensures reliability and reproducibility for your research applications.
SPECIFICATIONS
Specifications
C23H26IN7O2S • HCl
10 mg/ml in DMSO
100 nM - 10 μM
Negative (tested using EndotoxDetect™ assay)
In vitro cellular assays
Each lot is functionally tested and validated using cellular assays.
CONTENTS
Contents
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Product:BX795
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Cat code:tlrl-bx7
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Quantity:5 mg
BX795 is provided as a translucent film.
Shipping & Storage
- Shipping method: Room temperature
- -20°C
- Avoid repeated freeze-thaw cycles
Storage:
Caution:
Details
TBK1 /IKKε
TANK-binding kinase 1 (TBK1; also known as NF-κB activating kinase/NAK and T2K) is a multifunctional serine/threonine-protein kinase that belongs to the non-canonical IκB kinase family, together with its close homolog IkB kinase ε (IKKε, also known as IKKi). TBK1 plays an important role in the regulation of many cellular processes, including innate immunity, inflammatory cytokine production, autophagy, mitochondrial metabolism, and cell survival/proliferation [1].
In innate immune signaling, TBK1 acts as an integrator of receptor-mediated pathogen detection signals and as an interferon (IFN) response modulator [2, 3]. Viral, bacterial, or tumor DNA activate STING (stimulator of interferon genes protein), which triggers TBK1 signaling and results in the activation of the transcription factors IRF3 (IFN regulatory factor 3)and IRF7 to induce the expression of type-I IFNs. Additionally, TBK1 plays a role in other signaling pathways triggered by other innate adaptors, such as MAVS (mitochondrial antiviral signaling protein) and TRIF (TIR-domain-containing adapter-inducing interferon-β).
References:
1. Herhaus L., 2021. TBK1 (TANK-binding kinase 1)-mediated regulation of autophagy in health and disease. Matrix Biol. 100-101:84-98.
2. Durand J.K. et al., 2018. Roles for the IKK-related kinases TBK1 and IKKε in cancer. Cells. 7(9):139.
3. Runde AP. et al., 2022. The role of TBK1 in cancer pathogenesis and anticancer immunity J Exp Clin Cancer Res . 41(1):135.
Chemical structure of BX795
DOCUMENTS
Documents
Technical Data Sheet
Safety Data Sheet
Validation Data Sheet
Certificate of analysis
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