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 hydrochloride

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

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MRT68921 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    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.

    MRT68921 hydrochloride 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.

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    ULK1 ULK2

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    GSK-3 GSK-3α GSK-3β

    View All Bcl-2 Family Isoform Specific Products:

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

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    Description

    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[1][2].

    IC50 & Target[1][2]

    ULK2

    1.1 nM (IC50)

    ULK1

    2.9 nM (IC50)

    GSK-3β

     

    Bcl-2

     

    In Vitro

    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.

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

    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

    471.04

    Formula

    C25H35ClN6O
    CAS No.
    SMILES

    O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    MRT68921 hydrochloride Related Classifications

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      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:

    MRT689212070014-87-6MRT 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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