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BX 795
- Soluble in DMSO
- MF: C23H26IN7O2S
- MW: 591.47
Description
BX 795 is a potent inhibitor of TANK-binding kinase 1 (TBK1) and IKKε, with reported IC50 values of 6 nM and 41 nM, respectively; it also inhibits PDPK1 at higher concentration (IC50 value of 111 nM).
TBK1 and IKKε activate IRF3-dependent type I interferon signaling downstream of innate immune sensors. BX 795 is widely used to study antiviral signaling, inflammatory transcription and kinase-dependent interferon responses, although its broader kinase profile should be considered. The salt form, BX 795 hydrochloride (Axon 3350) is also available.
Key Features
- Potent TBK1 and IKKε inhibitor
- IC50: 6 nM (TBK1), 41 nM (IKKε) and 111 nM (PDPK1)
- Suppresses IRF3 and type I interferon pathway activation
- Useful innate-immunity tool with recognized off-target activity
Applications
- TBK1 and IKKε kinase assays
- cGAS–STING and RIG-I-like receptor signaling studies
- IRF3 phosphorylation and interferon-response research
- Antiviral and inflammatory pathway models
More Information
| Parent CAS No. | 702675-74-9 |
|---|---|
| Chemical Name | Pyrrolidine-1-carboxylic acid [3-(5-iodo-4-{3-[(thiophene-2-carbonyl)-amino]-propylamino}-pyrimidin-2-ylamino)-phenyl]-amide |
| SMILES | C1C(I)=C(NCCCNC(=O)C2=CC=CS2)N=C(NC2C=C(NC(=O)N3CCCC3)C=CC=2)N=1 |
| MFCD | MFCD12546134 |
| InChi | InChI=1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30) |
| InChiKey | VAVXGGRQQJZYBL-UHFFFAOYSA-N |
| CID | 10077147 |
| Short Description | PDK1/TBK1 inhibitor |
References
- R I Feldman et al. Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1. J. Biol. Chem., 2005, 280, 20, 19867-19874.
- J Bain et al. The selectivity of protein kinase inhibitors: a further update. Biochem. J. 2007, 408, 297–315.
- C Peifer, D R. Alessi, Small-Molecule Inhibitors of PDK1. ChemMedChem. 2008, 3 (12), 1810–1838.
- K Clark et al. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IκB kinase ϵ: a distinct upstream kinase mediates SER-172 phosphoylation and activation. J. Biol. Chem. 2009, 284, 14136-14146.
- List of publications using BX 795 (Axon 1390) purchased from Axon Medchem
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