MRT67307
Based on 29 publication(s) in Google Scholar
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.56%
- No. CAS: 1190378-57-4
- Fòrmula: C26H36N6O2
- Peso molecular:464.60
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Help & FAQs
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RU.521cGAS Inhibitor -
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Bafilomycin A1V-ATPase Inhibitor -
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RuxolitinibJAK1/2 Inhibitor -
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TBK1/IKKε-IN-2TBK1/IKKε Inhibitor -
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BMS-345541IKK-1/IKK-2 Inhibitor
Publications Citing Use of MedChemExpress (MCE) MRT67307
More- Nature. 2023 Mar;615(7950):158-167. [Abstract]
- Nat Med. 2018 Aug;24(8):1143-1150. [Abstract]
- Cell Res. 2019 Mar;29(3):193-205. [Abstract]
- Nat Cell Biol. 2025 Dec;27(12):2143-2151. [Abstract]
- Autophagy. 2026 Feb;22(2):316-329. [Abstract]
- Nat Commun. 2025 Jan 28;16(1):1109. [Abstract]
- Nat Commun. 2023 Sep 18;14(1):5666. [Abstract]
- Nat Commun. 2015 Jan 21:6:6074. [Abstract]
- Mol Cell. 2020 Dec 3;80(5):810-827.e7. [Abstract]
- Theranostics. 2018 Sep 9;8(17):4633-4648. [Abstract]
- Cell Chem Biol. 2022 Jul 21;29(7):1113-1125.e6. [Abstract]
- Int J Mol Med. 2018 Jul;42(1):248-258. [Abstract]
- Blood Adv. 2018 Dec 11;2(23):3428-3442. [Abstract]
- Mol Ther Methods Clin Dev. 2025 Jul 28;33(3):101542. [Abstract]
- Sci Rep. 2025 Dec 3. [Abstract]
- iScience. 2026 Jul 10;29(8):116736.
- Clin Immunol. 2026 Feb:283:110654. [Abstract]
- Biochem J. 2019 Mar 12;476(5):875-887. [Abstract]
- Mol Immunol. 2021 Mar:131:180-190. [Abstract]
- J Immunol Res. 2023 Mar 31:2023:5990156. [Abstract]
- bioRxiv. 2026 Mar 12.
- bioRxiv. 2025 Aug 21:2025.08.15.670603. [Abstract]
- bioRxiv. 2025 January 22.
- Patent. US20220305048A1.
- Patent. US20210025893A1.
- Patent. US20200246435A1.
- Harvard Medical School. 2018 June 13.
- Patent. US9814741B2.
- Patent. US20150202223A1.
Customer Validation & Images
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Cell Imaging/Staining
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Actividad biológica
Descripciòn
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TBK1 19 nM (IC50, at 0.1 mM ATP) |
IKKε 160 nM (IC50, at 0.1 mM ATP) |
ULK2 38 nM (IC50) |
ULK1 45 nM (IC50) |
Autophagy |
In Vitro
MRT67307 inhibits IKK and TBK1 with IC50 values of 160 and 19 nM when assayed at 0.1 mM ATP in vitro, but did not inhibit IKKα or IKKβ even at 10 μM[1].
MRT67307 (2 μM) prevents the phosphorylation of IRF3 in bone-marrow-derived macrophages (BMDMs). MRT67307 (2 μM) dose not suppresse the activation of JNK or p38 MAPK by poly(I:C)[1].
MRT67307 (1 nM-10 μM) prevents the production of IFNβ in macrophages[1].
MRT67307 (10 μM) is sufficient to reduce phospho-ATG13 to control levels[2].
MRT67307 (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs)[2].
MRT67307 (5 μM; 4 h) abrogates TBK1/IKKε-induced CYLD phosphorylation in 293T cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:293T cells
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Concentration:5 µM
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Incubation Time:4 hours
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Result:Abrogated TBK1/IKKε-induced CYLD phosphorylation.
Chemical Information
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No. CAS 1190378-57-4
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Appearance Solid
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Peso molecular 464.60
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Fòrmula C26H36N6O2
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Color Off-white to light yellow
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SMILES
O=C(NCCCNC1=NC(NC2=CC=CC(CN3CCOCC3)=C2)=NC=C1C4CC4)C5CCC5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (29)
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Journal Impact Factor
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Most Recent
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Nature
2023 Mar;615(7950):158-167. PMID: 36634707 -
Nat Med
2018 Aug;24(8):1143-1150. PMID: 30038220
MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Med. 2018 Aug;24(8):1143-1150. [Abstract]
Immunoblot of pSTAT1, STAT1 and β-actin levels in H69AR cells±200 ng/mL IFNg 10 min pulse followed by 24 h chase in media with DMSO, Ruxolitinib (100 nM) or MRT67307 (1 µM).
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Cell Res
Virus-induced accumulation of intracellular bile acids activates the TGR5-β-arrestin-SRC axis to enable innate antiviral immunity. [Abstract]2019 Mar;29(3):193-205. PMID: 30651583 -
Nat Cell Biol
DNA fragmentation factor B suppresses interferon to enable cancer persister cell regrowth. [Abstract]2025 Dec;27(12):2143-2151. PMID: 41249572
MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2025 Dec;27(12):2143-2151. [Abstract]
Total STAT1 levels in A375 persister cells cotreated for 14 days with 1 μM TBK1 inhibitor MRT67307 (TBK1i) or 1 μM JAKi.
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Autophagy
Regulation of pexophagy by a novel TBK1-MARCHF7-PXMP4-NBR1 axis in PEX1-depleted HeLa cells. [Abstract]2026 Feb;22(2):316-329. PMID: 41267209 -
Nat Commun
Activation of lysophagy by a TBK1-SCFFBXO3-TMEM192-TAX1BP1 axis in response to lysosomal damage. [Abstract]2025 Jan 28;16(1):1109. PMID: 39875384
MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 28;16(1):1109. [Abstract]
HepG2/GFP-Gal3 cells were treated with either MRT67307 (2 µM) or GSK8612 (10 µM) in combination with LLOMe (750 µM). After the 2-h treatment, LLOMe was washed out with normal cell culture media, and the cells were further incubated with either MRT67307 or GSK8612 for 24 h. The number of GFP-Gal3 puncta was quantified.
MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 28;16(1):1109. [Abstract]
HepG2 cells were transfected with both HA-ubiquitin and TMEM192-FLAG and pretreated with either MRT67307 (MRT, 2 µM) or GSK8612 (10 µM). LLOMe was cotreated for an additional 2 h. Subsequently, the cells were immunoprecipitated with agarose bead-conjugated anti-FLAG antibody and further analyzed by western blotting using the indicated antibodies. The results demonstrate that treatment with the TBK1 inhibitor MRT67307 (MRT) attenuated the LLOMe-induced increase in TMEM192 ubiquitination levels.
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Nat Commun
Pharmacological inhibition of TBK1/IKKε blunts immunopathology in a murine model of SARS-CoV-2 infection. [Abstract]2023 Sep 18;14(1):5666. PMID: 37723181 -
Nat Commun
Regulation of T-cell activation and migration by the kinase TBK1 during neuroinflammation. [Abstract]2015 Jan 21:6:6074. PMID: 25606824
MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2015 Jan 21:6:6074. [Abstract]
MRT67307 efficiently inhibited the AKT degradation. IB analysis using WT CD4+ T cells, pretreated for 1 h with a TBK1 inhibitor, MRT67307, of solvent control DMSO and subsequently stimulated for the indicated times with anti-CD3 plus anti-CD28 in the presence of a protein synthesis inhibitor, Cycloheximide.
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Mol Cell
TBK1-Mediated DRP1 Targeting Confers Nucleic Acid Sensing to Reprogram Mitochondrial Dynamics and Physiology. [Abstract]2020 Dec 3;80(5):810-827.e7. PMID: 33171123 -
Theranostics
Aphthous ulcer drug inhibits prostate tumor metastasis by targeting IKKɛ/TBK1/NF-κB signaling. [Abstract]2018 Sep 9;8(17):4633-4648. PMID: 30279728 -
Cell Chem Biol
Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599 -
Int J Mol Med
Quercetin inhibits NTHi-triggered CXCR4 activation through suppressing IKKα/NF-κB and MAPK signaling pathways in otitis media. [Abstract]2018 Jul;42(1):248-258. PMID: 29568908 -
Blood Adv
The kinases IKBKE and TBK1 regulate MYC-dependent survival pathways through YB-1 in AML and are targets for therapy. [Abstract]2018 Dec 11;2(23):3428-3442. PMID: 30504235 -
Mol Ther Methods Clin Dev
Enhanced B cell electroporation efficiency via inhibition of DNA-induced apoptosis and pyroptosis with pan-caspase inhibitor. [Abstract]2025 Jul 28;33(3):101542. PMID: 40821855 -
Sci Rep
Pseudomonas aeruginosa-derived DnaJ functions as a novel immunomodulator inducing IFNβ via CME-SGK1-IRF3 axis in macrophages. [Abstract]2025 Dec 3. PMID: 41339751 -
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Clin Immunol
Development and validation of a flow cytometry-based ISG15 induction assay to monitor the type I interferon response. [Abstract]2026 Feb:283:110654. PMID: 41344526 -
Biochem J
Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2). [Abstract]2019 Mar 12;476(5):875-887. PMID: 30782972 -
Mol Immunol
DNA damage-triggered activation of cGAS-STING pathway induces apoptosis in human keratinocyte HaCaT cells. [Abstract]2021 Mar:131:180-190. PMID: 33423764 -
J Immunol Res
c-Myb Dominates TBK1-Mediated Endotoxin Tolerance in Kupffer Cells by Negatively Regulating DTX4. [Abstract]2023 Mar 31:2023:5990156. PMID: 37032653 -
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bioRxiv
2025 Aug 21:2025.08.15.670603. PMID: 40894800 -
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Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (215.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Clark K, et al. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104. [Content Brief]
[2]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [Content Brief]
[3]. Zhu Z, et al. Inhibition of KRAS-driven tumorigenicity by interruption of an autocrine cytokine circuit. 26.37Cancer Discov. 2014 Apr;4(4):452-65. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1524 mL | 10.7619 mL | 21.5239 mL | 53.8097 mL |
| 5 mM | 0.4305 mL | 2.1524 mL | 4.3048 mL | 10.7619 mL | |
| 10 mM | 0.2152 mL | 1.0762 mL | 2.1524 mL | 5.3810 mL | |
| 15 mM | 0.1435 mL | 0.7175 mL | 1.4349 mL | 3.5873 mL | |
| 20 mM | 0.1076 mL | 0.5381 mL | 1.0762 mL | 2.6905 mL | |
| 25 mM | 0.0861 mL | 0.4305 mL | 0.8610 mL | 2.1524 mL | |
| 30 mM | 0.0717 mL | 0.3587 mL | 0.7175 mL | 1.7937 mL | |
| 40 mM | 0.0538 mL | 0.2690 mL | 0.5381 mL | 1.3452 mL | |
| 50 mM | 0.0430 mL | 0.2152 mL | 0.4305 mL | 1.0762 mL | |
| 60 mM | 0.0359 mL | 0.1794 mL | 0.3587 mL | 0.8968 mL | |
| 80 mM | 0.0269 mL | 0.1345 mL | 0.2690 mL | 0.6726 mL | |
| 100 mM | 0.0215 mL | 0.1076 mL | 0.2152 mL | 0.5381 mL |
MRT67307 Related Classifications
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