2. Autophagy NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis Stem Cell/Wnt PI3K/Akt/mTOR
  3. ULK Reactive Oxygen Species (ROS) Apoptosis GSK-3 Bcl-2 Family
  4. MRT68921

MRT68921 is a potent NUAK1/ULK1 dual inhibitor. MRT68921 inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 can be used for the research of cancer, such as breast cancer.

For research use only. We do not sell to patients.

CAS No. : 1190379-70-4

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of MRT68921:

MRT68921 Related Antibodies

Top Publications Citing Use of Products

    MRT68921 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 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.

    MRT68921 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.

    MRT68921 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.

    MRT68921 purchased from MedChemExpress. Usage Cited in: Mol Ther Oncolytics. 2021 Aug 28:23:107-123.

    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.

    View All ULK Isoform Specific Products:

    View All Isoforms
    ULK1 ULK2

    View All GSK-3 Isoform Specific Products:

    View All Isoforms
    GSK-3 GSK-3α GSK-3β

    View All Bcl-2 Family Isoform Specific Products:

    View All Isoforms
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MRT68921 is a potent NUAK1/ULK1 dual inhibitor. MRT68921 inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 can be used for the research of cancer, such as breast cancer[1][2].

    IC50 & Target[1][2]

    ULK2

    1.1 nM (IC50)

    ULK1

    2.9 nM (IC50)

    GSK-3β

     

    Bcl-2

     

    In Vitro

    MRT68921 (1 μM, 1 h) reduces basal LC3 puncta and blocks basal autophagy in mouse embryonic fibroblasts (MEFs)[1].
    MRT68921 (1 μM) reduces LC3-II levels in TBK1 knock-out and matched wild-type MEFs[1].
    MRT68921 (24 h) exhibits cytotoxic activity in cancer cells with IC50 values ranging from 1.76-8.91 μM[2].
    MRT68921 (0-10 μM, 8-24 h) induces ROS production and apoptosis in NCI-H460 and MNK45 cells[2].
    MRT68921 (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.

    MRT68921 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: U251 and MNK45 cells
    Concentration: 0, 0.5, 1, 2, 3 and 5 μM
    Incubation Time: 8 h
    Result: Increased cleaved PARP1 expression.
    Downregulated phosphorylation of MYPT1 and Gsk3β.
    Increased puncta LC3.
    In Vivo

    MRT68921 (10-40 mg/kg, s.c., daily for 7 times) inhibits tumor growth in NCI-H460 tumor mice models[2].
    MRT68921 (20 mg/kg, s.c., every 2 days for 7 times) inhibits tumor growth in MNK45 tumor mice models[2].
    MRT68921 (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.

    Animal Model: NCI-H460 tumor mice models[2]
    Dosage: 10, 20, or 40 mg/kg
    Administration: Subcutaneously injection, daily for 7 times
    Result: Reduced tumor volume.
    Increased Bax levels and decreased Bcl-2 levels.
    Animal Model: MNK45 tumor mice models[2]
    Dosage: 20 mg/kg
    Administration: Subcutaneously injection, every 2 days for 7 times
    Result: Reduced tumor volume.
    Animal Model: 4T1 tumor mice models[2]
    Dosage: 20 mg/kg
    Administration: Intraperitoneally injection, daily for 7 times
    Result: Reduced the number of lung metastatic nodules.
    Had no abnormal structures of the heart, kidney, liver, and spleen.
    Molecular Weight

    434.58

    Formula

    C25H34N6O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (230.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3011 mL 11.5054 mL 23.0107 mL
    5 mM 0.4602 mL 2.3011 mL 4.6021 mL
    View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (5.75 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.75 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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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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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation
    References

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3011 mL 11.5054 mL 23.0107 mL 57.5268 mL
    5 mM 0.4602 mL 2.3011 mL 4.6021 mL 11.5054 mL
    10 mM 0.2301 mL 1.1505 mL 2.3011 mL 5.7527 mL
    15 mM 0.1534 mL 0.7670 mL 1.5340 mL 3.8351 mL
    20 mM 0.1151 mL 0.5753 mL 1.1505 mL 2.8763 mL
    25 mM 0.0920 mL 0.4602 mL 0.9204 mL 2.3011 mL
    30 mM 0.0767 mL 0.3835 mL 0.7670 mL 1.9176 mL
    40 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
    50 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1505 mL
    60 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
    80 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
    100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
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    MRT68921 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MRT689211190379-70-4MRT 68921MRT-68921ULKReactive Oxygen Species (ROS)ApoptosisGSK-3Bcl-2 FamilyUnc-51 like kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3NUAK1ROSLC3GSK3Bcl-2Breast cancerNCI-H460MNK45Inhibitorinhibitorinhibit

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