fbpx

BX 795 | TBK1 Inhibitor

$115.00$350.00

BX 795 is a potent TBK1 inhibitor that has been fully validated with Human TBK1 using the Transcreener ADP Assay. An IC50 of 2.25 nM was obtained using a 12-point dose-response assay. Contact us for bulk sizes.

SKU: 5001-5mg , 5001-25mg Category: Tag:

Technical Data for BX 795

Functional Activity with Human TBK1

Activity was measured using the Transcreener® ADP2 FP Assay using 4 nM human TBK1 (SignalChem #T02-10G). BX 795 was serially diluted and incubated with enzyme for 30 minutes. The following was added to start the reaction: 10 µM ATP, 10 µM CK1tide, 25 mM TRIS pH 7.5, 2.5 mM MgCl2, 0.01% Triton X-100; 10 μL Enzyme Reaction incubated @ 30°C for 60 minutes in a Corning® low-volume 384-well plate (#4514). 10 μL of the following detect mix was added: 18 μg/ mL ADP2 Ab, 4 nM ADP2 Tracer, 1X Stop and Detect Buffer B. 20 μL Complete Reaction was incubated for 60 minutes and read on a CLARIOstarPlus instrument. Fluorescent Polarization values were converted to ADP formed with a 10 μM ADP Standard Curve and was plotted using Prism (GraphPad). An IC50 of 2.25 nM was obtained.

TBK1 Dose Response with BX 795

TBK1 Assay Dose Response with BX-975 Inhibitor

IC50 = 2.25 nM

Learn More About the Transcreener ADP TBK1 Assay to Measure BX 795 Inhibition

Detailed Description

BX 795, 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 ERK83. Exhibited antitumor activity in human oral squamous cell carcinoma4, pancreatic ductal adenocarcinoma5, and Glioblastoma Multiforme6. BX 795 has been used to enhance lentiviral transduction efficiency in human NK cells7-9 and human primary T cells10 for CAR-T cell therapy.

Contact Our Team Today

Interested in a bulk order or have a question about the product? Please fill out the form below and a BellBrook team member will follow-up quickly. 

References

  1. Feldman et al. (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1; J. Biol. Chem. 280 198672) Bain et al. (2007) The selectivity of protein kinase inhibitors: a further update; Biochem. J. 408 297
  2. 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
  3. 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
  4. 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
  5. Scuderi et al. (2021) TBK1 Inhibitor Exerts Antiproliferative Effect on Glioblastoma Multiforme Cells; Oncol. Res. 28 779
  6. 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
  7. 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
  8. 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
  9. 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
TOP