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Kinase inhibitor; 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) . 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 . Additionally, MRT67307 is a highly potent inhibitor of ULK1, a key component of the autophagy pathway .
- MRT67307 potently inhibits IRF signaling in a dose-dependent manner.
- MRT67307 does not affect NF-κB signaling.
- Each lot of MRT67307 is functionally tested.
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.
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
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.
CAS number: 1190378-57-4
Solubility: 15 mg/ml in H2O
Working concentration: 1 µM to 20 μM for cell culture assays
Formula: C26H36N6O2 . x HCl
Molecular weight: 464.60 g/mol
- 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.
- 10 mg MRT67307 (hydrochloride) provided as a dried powder
MRT67307 is shipped at room temperature.
Upon receipt, store product at -20 °C. Upon resuspension of MRT67307 prepare aliquots and store at -20 °C.
Resuspended product is stable for at least 3 months when properly stored.
Avoid repeated freeze-thaw cycles.Back to the top
Chemical structure of MRT67307:
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