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MRT67307

MRT67307 Unit size Cat. code Docs Qty Price
Kinase inhibitor; TBK1 and IKKε inhibitor
10 mg
inh-mrt
+-
$177.00

NEW PRODUCT

TBK1/IKKε inhibitor

MRT67307 is a potent, reversible kinase inhibitor specifically blocking the function of TBK1 (TANK-binding kinase 1) and I-kappa-B kinase (IKK) epsilon (IKKε, or IKBKE), thereby preventing the phosphorylation of IRF3 (interferon regulatory factor 3) and subsequent expression of interferon-stimulated genes (ISGs)  [1]. Unlike BX795 from which it is derived, MRT67307 has no noted effect on the canonical IKKs, IKKα or IKKβ, that are involved in the activation of NF-κB [1]. Additionally, MRT67307 is a highly potent inhibitor of ULK1, a key component of the autophagy pathway [2].

  • MRT67307 potently inhibits IRF signaling in a dose-dependent manner.
  • MRT67307 does not affect NF-κB signaling.
  • Each lot of MRT67307 is functionally tested.


References:

1. Clark, K. et al., 2011. Novel cross-talk within the IKK family controls innate immunity. Biochem J 434, 93-104.
2. Petherick, K.J. et al., 2015. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem 290, 11376-11383.

Figures

Inhibition of 3p-hpRNA and 2’3-cGAMP-induced responses in THP1-Dual™ Cells
Inhibition of 3p-hpRNA and 2’3-cGAMP-induced responses in THP1-Dual™ Cells

2x105 THP1-Dual™ cells were transfected with 1 μg/ml 3p-hpRNA/LyoVec™ or incubated with 30 μg/ml 2’3’-cGAMP in the presence or absence of increasing concentrations of MRT67307. After overnight incubation, activation of IRF was assessed by measuring Lucia luciferase activity in the supernatant, using QUANTI-Luc™ detection reagent. Percentages of the maximal response for the ligand with no inhibitor are shown

Inhibition of 3p-hpRNA-induced responses in THP1-Dual™ Cells
Inhibition of 3p-hpRNA-induced responses in THP1-Dual™ Cells

2x105 THP1-Dual™ cells were transfected with 1 μg/ml 3p-hpRNA/LyoVec™ with or without 1 μg/ml BX795 or 3 μg/ml MRT67307. After overnight incubation, activation of IRF was assessed by measuring Lucia luciferase activity in the supernatant using QUANTI-Luc™ detection reagent. Percentages of the maximal response for the ligand with no inhibitor are shown on the left axis. The activation NF-κB was assessed by measuring SEAP activity in the supernatant using QUANTI-Blue™ Solution detection reagent. OD at 630 nm are shown on the right axis.

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Specifications

CAS number: 1190378-57-4

Solubility: 15 mg/ml in H2O

Working concentration:  1 µM to 20 μM for cell culture assays

Formula: C26H36N6O. x HCl

Molecular weight: 464.60 g/mol

Quality control:

  • Purity: ≥95% (UHPLC)
  • Inhibition of TBK1/IKKε by MRT67307 has been confirmed using cellular assays.
  • Absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ hTLR2 and HEK-Blue™ hTLR4 cells.
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Contents

  • 10 mg MRT67307 (hydrochloride) provided as a dried powder

Room temperature MRT67307 is shipped at room temperature.

Store Upon receipt, store product at -20 °C. Upon resuspension of MRT67307 prepare aliquots and store at -20 °C.

Stability Resuspended product is stable for at least 3 months when properly stored.

Alert Avoid repeated freeze-thaw cycles.

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Details

Chemical structure of MRT67307:

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