MRT68921 hydrochloride
Based on 28 publication(s) in Google Scholar
MRT68921 hydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 hydrochloride inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 hydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 hydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 hydrochloride can be used for the research of cancer, such as breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2070014-87-6
- Formula: C25H35ClN6O
- Molecular Weight:471.04
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MRT68921 hydrochloride
More- Nature. 2022 Oct;610(7931):366-372. [Abstract]
- Cancer Cell. 2021 May 10;39(5):678-693.e11. [Abstract]
- Nat Cancer. 2021 May;2(5):503-514. [Abstract]
- Nat Cell Biol. 2026 Apr;28(4):812-827. [Abstract]
- ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]
- Nat Commun. 2025 Nov 19;16(1):10181. [Abstract]
- Dev Cell. 2025 Jun 27:S1534-5807(25)00372-7. [Abstract]
- Dev Cell. 2024 Jan 22;59(2):228-243.e7. [Abstract]
- J Ethnopharmacol. 2024 Aug 3:118658. [Abstract]
- Mol Ther Oncolytics. 2021 Aug 28:23:107-123. [Abstract]
- PLoS Pathog. 2024 Aug 13;20(8):e1012461. [Abstract]
- Bioorg Chem. 2024 Jun:147:107412. [Abstract]
- Biochem J. 2019 Mar 12;476(5):875-887. [Abstract]
- FASEB J. 2026 Jan 31;40(2):e71454. [Abstract]
- J Cell Physiol. 2021 Dec;236(12):8110-8121. [Abstract]
- Sci Rep. 2023 Jul 3;13(1):10752. [Abstract]
- Med Oncol. 2026 Mar 3;43(4):163. [Abstract]
- Mol Med Rep. 2024 Apr;29(4):67. [Abstract]
- mSphere. 2025 Jan 10:e0053724. [Abstract]
- Vet Microbiol. 2026 May:316:110993. [Abstract]
- bioRxiv. 2026 Apr 5.
- SSRN. 2025 Jul 25.
- bioRxiv. 2025 Jun 5:2025.05.29.656904. [Abstract]
- Res Sq. 2025 May 07.
- Medical University of South Carolina. 2023 Aug 12.
- Research Square Preprint. 2023 May 22.
- Patent. US20230068698A1.
- Research Square Preprint. 2021 Oct.
Customer Validation & Images
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Biological Activity
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ULK2 1.1 nM (IC50) |
ULK1 2.9 nM (IC50) |
GSK-3β |
Bcl-2 |
MRT68921 hydrochloride (1 μM, 1 h) reduces basal LC3 puncta and blocks basal autophagy in mouse embryonic fibroblasts (MEFs)[1].
MRT68921 hydrochloride (1 μM) reduces LC3-II levels in TBK1 knock-out and matched wild-type MEFs[1].
MRT68921 hydrochloride (24 h) exhibits cytotoxic activity in cancer cells with IC50 values ranging from 1.76-8.91 μM[2].
MRT68921 hydrochloride (0-10 μM, 8-24 h) induces ROS production and apoptosis in NCI-H460 and MNK45 cells[2].
MRT68921 hydrochloride (0-5 μM, 8h) suppresses the NUAK1/MYPT1/Gsk3β andautophagy associated signaling pathway in U251 and MNK45 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U251 and MNK45 cells
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Concentration:0, 0.5, 1, 2, 3 and 5 μM
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Incubation Time:8 h
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Result:Increased cleaved PARP1 expression.
Downregulated phosphorylation of MYPT1 and Gsk3β.
Increased puncta LC3.
MRT68921 hydrochloride (20 mg/kg, s.c., every 2 days for 7 times) inhibits tumor growth in MNK45 tumor mice models[2].
MRT68921 hydrochloride (20 mg/kg, i.p., daily for 7 times) reduces the number of lung metastatic nodules in 4T1 tumor mice models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H460 tumor mice models[2]
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Dosage:10, 20, or 40 mg/kg
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Administration:Subcutaneously injection, daily for 7 times
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Result:Reduced tumor volume.
Increased Bax levels and decreased Bcl-2 levels.
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Animal Model:MNK45 tumor mice models[2]
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Dosage:20 mg/kg
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Administration:Subcutaneously injection, every 2 days for 7 times
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Result:Reduced tumor volume.
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Animal Model:4T1 tumor mice models[2]
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Dosage:20 mg/kg
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Administration:Intraperitoneally injection, daily for 7 times
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Result:Reduced the number of lung metastatic nodules.
Had no abnormal structures of the heart, kidney, liver, and spleen.
Chemical Information
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CAS No. 2070014-87-6
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Molecular Weight 471.04
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Formula C25H35ClN6O
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SMILES
O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
2022 Oct;610(7931):366-372. PMID: 36198801 -
Cancer Cell
2021 May 10;39(5):678-693.e11. PMID: 33740421 -
Nat Cancer
ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer. [Abstract]2021 May;2(5):503-514. PMID: 34142094 -
Nat Cell Biol
TOLLIP targets GSDME-NT-carrying endocytic vesicles for autophagy to regulate pyroptosis and chemotherapy efficacy. [Abstract]2026 Apr;28(4):812-827. PMID: 41803502 -
ACS Nano
Realistic Nanoplastics Induced Pulmonary Damage via the Crosstalk of Ferritinophagy and Mitochondrial Dysfunction. [Abstract]2024 Jul 2;18(26):16790-16807. PMID: 38869479
MRT68921 hydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]
TC-1 cells were pretreated with 1 μM MRT68921 for 1 h, followed by NP treatment for 24 h. MRT68921 inhibited the upregulation of NP-induced p-ULK1, ATG5, and LC3-II and the downregulation of SQSTM1 and GPX4.
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Nat Commun
PRDX1 promotes testosterone synthesis and attenuates aging via redox regulation of ATG4B to modulate lipophagy. [Abstract]2025 Nov 19;16(1):10181. PMID: 41261096 -
Dev Cell
2025 Jun 27:S1534-5807(25)00372-7. PMID: 40609542
MRT68921 hydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2025 Jun 27:S1534-5807(25)00372-7. [Abstract]
Confocal images of mCherry-GOLPH3-expressing U2OS cells. Cells were either untreated or treated with EBSS for 12 hours, in the presence or absence of MRT68921 (250 μM). Right: Quantification of the percentage of cells with dispersed mCherry-GOLPH3. A total of 300 cells for each sample were quantified. n = 3. Scale bar: 10 µm.
MRT68921 hydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2025 Jun 27:S1534-5807(25)00372-7. [Abstract]
Inhibition of EBSS-induced mCherry-GOLPH3 cleavage by ULK1 inhibitor MRT68921 (250 μM). U2OS cells transfected with the mCherry-GOLPH3 plasmid were left untreated or treated with EBSS, in the presence or absence of MRT68921 for 8 hours.
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Dev Cell
Autophagy supports PDGFRA-dependent brain tumor development by enhancing oncogenic signaling. [Abstract]2024 Jan 22;59(2):228-243.e7. PMID: 38113891 -
J Ethnopharmacol
2024 Aug 3:118658. PMID: 39103023
MRT68921 hydrochloride purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2024 Aug 3:118658. [Abstract]
MRT68921 (MRT, 5 μM; 2 h) attenuates the accumulation of LC3-II, thereby reducing YB treatment-induced necroptosis.
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Mol Ther Oncolytics
Oleanolic acid blocks the purine salvage pathway for cancer therapy by inactivating SOD1 and stimulating lysosomal proteolysis. [Abstract]2021 Aug 28:23:107-123. PMID: 34703880
MRT68921 hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Ther Oncolytics. 2021 Aug 28:23:107-123. [Abstract]
The effects of two ULK1 inhibitors, ULK-101 (1 μM) and MRT68921 (1 μM), on levels of phospho-ATG14 (Ser29), ATG14, LC3-I/II, HGPRT, and 5′-NT in OA-treated A549 cells. The results showed that both ULK1 inhibitors rapidly downregulated phosphorylated ATG14 at Ser29, a well-established substrate of ULK1, reduced LC3-II isoform expression, and stabilized HGPRT and 5′-N.
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PLoS Pathog
A small protein encoded by PCBP1-AS1 is identified as a key regulator of influenza virus replication via enhancing autophagy. [Abstract]2024 Aug 13;20(8):e1012461. PMID: 39137200 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
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 -
FASEB J
EM2, a Novel Elephantopus mollis H.B.K. Monomer, Enhances Radiosensitivity in Cervical Cancer Through Dual Inhibition of AKT and Autophagy. [Abstract]2026 Jan 31;40(2):e71454. PMID: 41527777 -
J Cell Physiol
2021 Dec;236(12):8110-8121. PMID: 34101831 -
Sci Rep
2023 Jul 3;13(1):10752. PMID: 37400460 -
Med Oncol
ULK1-driven autophagy modulation alters tumor-promoting pathways in triple-negative breast cancer. [Abstract]2026 Mar 3;43(4):163. PMID: 41774346 -
Mol Med Rep
2024 Apr;29(4):67. PMID: 38456519 -
mSphere
Inhibition of Unc-51-like-kinase is mitoprotective during Pseudomonas aeruginosa infection in corneal epithelial cells. [Abstract]2025 Jan 10:e0053724. PMID: 39791872 -
Vet Microbiol
Porcine reproductive and respiratory syndrome virus nsp2 protects viral RNA-dependent RNA polymerase from autophagic degradation. [Abstract]2026 May:316:110993. PMID: 41861694 -
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bioRxiv
2025 Jun 5:2025.05.29.656904. PMID: 40501952 -
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Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
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- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. 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]
[2]. Chen Y, et al. Dual targeting of NUAK1 and ULK1 using the multitargeted inhibitor MRT68921 exerts potent antitumor activities. Cell Death Dis. 2020 Sep 1;11(8):712. [Content Brief]
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