MRT67307 hydrochloride
Based on 28 publication(s) in Google Scholar
MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2095432-39-4
- Formel: C26H37ClN6O2
- Molecular Weight:501.06
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) MRT67307 hydrochloride
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. 2025 Nov 27:1-14. [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 advances. 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]
- Clin Immunol. 2025 Dec 2:283:110654. [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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Biologische Aktivität
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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 |
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.
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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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CAS. Nr. 2095432-39-4
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Molecular Weight 501.06
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Formel C26H37ClN6O2
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SMILES
O=C(C1CCC1)NCCCNC2=NC(NC3=CC=CC(CN4CCOCC4)=C3)=NC=C2C5CC5.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (28)
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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 hydrochloride 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 hydrochloride 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]2025 Nov 27:1-14. 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 advances
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 -
Clin Immunol
Development and validation of a flow cytometry-based ISG15 induction assay to monitor the type I interferon response. [Abstract]2025 Dec 2:283:110654. 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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Reinheit & Dokumentation
Verweise
[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]
Calculators
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