BX795 | Dual TBK1/IKKε inhibitor – enhances lentiviral transduction efficiency
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Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $65.00 | ||
| 25 mg | $250.00 |
BX795 (702675-74-9), originally described as a moderately potent inhibitor of PDK1 (IC50 = 111 nM)1, is, more importantly, a dual inhibitor of TBK1 and IKKε (IC50’s = 6 and 41 nM respectively)2. TBK1 and IKKε regulate the production of Type I interferons during bacterial and viral infection via phosphorylation of the transcription factor IRF3. It also inhibited of MARK, MLK, NUAK, AurB, and ERK8.3 BX795 exhibited antitumor activity in human oral squamous cell carcinoma4, pancreatic ductal adenocarcinoma5, and Glioblastoma Multiforme6. BX795 has been used to enhance lentiviral transduction efficiency in human NK cells7-9 and human primary T cells10 for CAR-T cell therapy.
References/Citations:
- Feldman et al. (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1; J. Biol. Chem. 280 19867
- Bain et al. (2007) The selectivity of protein kinase inhibitors: a further update; Biochem. J. 408 297
- Clark et al. (2009) Use of the Pharmacological Inhibitor BX795 to Study the Regulation and Physiological Roles of TBK1 and IkB Kinase ε; J. Biol. Chem. 284 14136
- Bai et al. (2015) BX795, a TBK1 inhibitor, exhibits antitumor activity in human oral squamous cell carcinoma through apoptosis induction and mitotic phase arrest; Eur. J. Pharmacol. 769 287
- Choi et al. (2019) A pharmacogenomic analysis using L1000CDS2 identifies BX-795 as a potential anticancer drug for primary pancreatic ductal adenocarcinoma cells; Cancer Lett. 465 82
- Scuderi et al. (2021) TBK1 Inhibitor Exerts Antiproliferative Effect on Glioblastoma Multiforme Cells; Oncol. Res. 28 779
- Sutlu et al. (2012) Inhibition of Intracellular Antiviral Defense Mechanisms Augments Lentiviral Transduction of Human Natural Killer Cells: Implications for Gene Therapy; Hum. Gene Ther. 23 1090
- Allan et al. (2021) Systematic improvements in lentiviral transduction of primary human natural killer cells undergoing e4x vivo expansion; Mol. Ther. Methods Clin. Dev. 20 559
- Chockley et al. (2021) Transient blockade of TBK1/IKKε allows efficient transduction of primary human natural killer cells with vesicular stomatitis virus G-pseudotyped lentiviral vectors; Cytotherapy 23 787
- Lingyu et al. (2020) Lentiviral delivery of combinatorial CAR/CRISPRi circuit into human primary T cells is enhanced by TBK1/IKKε complex inhibitor BX795; J. Transl. Med. 18 363
NMR (Conforms)
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Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
BX795 (702675-74-9), originally described as a moderately potent inhibitor of PDK1 (IC50 = 111 nM)1, is, more importantly, a dual inhibitor of TBK1 and IKKε (IC50’s = 6 and 41 nM respectively)2. TBK1 and IKKε regulate the production of Type I interferons during bacterial and viral infection via phosphorylation of the transcription factor IRF3. It also inhibited of MARK, MLK, NUAK, AurB, and ERK8.3 BX795 exhibited antitumor activity in human oral squamous cell carcinoma4, pancreatic ductal adenocarcinoma5, and Glioblastoma Multiforme6. BX795 has been used to enhance lentiviral transduction efficiency in human NK cells7-9 and human primary T cells10 for CAR-T cell therapy.
References/Citations:
- Feldman et al. (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1; J. Biol. Chem. 280 19867
- Bain et al. (2007) The selectivity of protein kinase inhibitors: a further update; Biochem. J. 408 297
- Clark et al. (2009) Use of the Pharmacological Inhibitor BX795 to Study the Regulation and Physiological Roles of TBK1 and IkB Kinase ε; J. Biol. Chem. 284 14136
- Bai et al. (2015) BX795, a TBK1 inhibitor, exhibits antitumor activity in human oral squamous cell carcinoma through apoptosis induction and mitotic phase arrest; Eur. J. Pharmacol. 769 287
- Choi et al. (2019) A pharmacogenomic analysis using L1000CDS2 identifies BX-795 as a potential anticancer drug for primary pancreatic ductal adenocarcinoma cells; Cancer Lett. 465 82
- Scuderi et al. (2021) TBK1 Inhibitor Exerts Antiproliferative Effect on Glioblastoma Multiforme Cells; Oncol. Res. 28 779
- Sutlu et al. (2012) Inhibition of Intracellular Antiviral Defense Mechanisms Augments Lentiviral Transduction of Human Natural Killer Cells: Implications for Gene Therapy; Hum. Gene Ther. 23 1090
- Allan et al. (2021) Systematic improvements in lentiviral transduction of primary human natural killer cells undergoing e4x vivo expansion; Mol. Ther. Methods Clin. Dev. 20 559
- Chockley et al. (2021) Transient blockade of TBK1/IKKε allows efficient transduction of primary human natural killer cells with vesicular stomatitis virus G-pseudotyped lentiviral vectors; Cytotherapy 23 787
- Lingyu et al. (2020) Lentiviral delivery of combinatorial CAR/CRISPRi circuit into human primary T cells is enhanced by TBK1/IKKε complex inhibitor BX795; J. Transl. Med. 18 363
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