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BX795

BX795 Unit size Cat. code Docs Qty Price
TBK1/IKKε inhibitor
5 mg
tlrl-bx7
+-
$171.00

TBK1/IKKε inhibitor

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].

It was recently shown to be 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].

 

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.

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Specifications

CAS number: 702675-74-9

Working concentration: 100 nM - 10 μM

Solubility: DMSO (10 mg/ml)

Formula: C23H26IN7O2S

Molecular weight: 591.5

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Contents

BX795 is provided as a translucent film.

  • 5 mg BX795

BX795 is shipped at room temperature.

Store at -20°C.

Solid product is stable for 1 year at -20°C.

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Details

B16-Blue IFN-alpha/beta cells were incubated with varying concentrations of BX795

B16-Blue™  IFN-α/β cells were incubated for 6h with varying concentrations of BX795 prior to overnight stimulation with 1µg/ml of 5'ppp-dsRNA or 1.10e4 U/ml mIFN-α.
Levels of reporter SEAP protein in the supernatant were mesured at O.D. 655nm after incubation with QUANTI-Blue™.

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Citations

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