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

MRT68921 dihydrochloride 是一种强效的 NUAK1/ULK1 双重抑制剂。MRT68921 dihydrochloride 抑制 ULK1 和 ULK2 的 IC50 值分别为 2.9 nM 和 1.1 nM。MRT68921 dihydrochloride 可通过打破氧化应激信号的平衡来阻断细胞自噬并杀死肿瘤细胞。MRT68921 dihydrochloride能够抑制细胞增殖，诱导活性氧 (ROS) 的产生和细胞凋亡 (apoptosis)。MRT68921 dihydrochloride 可用于癌症研究，如乳腺癌。

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CAS No. : 2080306-21-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥670
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1 mg ￥274
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5 mg ￥600
In-stock
10 mg ￥1000
In-stock
25 mg ￥2200
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50 mg ￥3900
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100 mg ￥5400
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Customer Review

Other Forms of MRT68921 dihydrochloride:

MRT68921 dihydrochloride 相关抗体

Top Publications Citing Use of Products

    MRT68921 dihydrochloride purchased from MCE. 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 dihydrochloride purchased from MCE. 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 dihydrochloride purchased from MCE. 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 dihydrochloride purchased from MCE. 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 dihydrochloride purchased from MCE. 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.

    查看 ULK 亚型特异性产品:

    查看所有亚型
    ULK1 ULK2

    查看 GSK-3 亚型特异性产品:

    查看所有亚型
    GSK-3 GSK-3α GSK-3β

    查看 Bcl-2 Family 亚型特异性产品:

    查看所有亚型
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

     

    体外研究
    (In Vitro)

    MRT68921 dihydrochloride (1 μM, 1 h) 可减少小鼠胚胎成纤维细胞 (MEFs) 中的基础 LC3 斑点并阻断基础自噬[1]。
    MRT68921 dihydrochloride (1 μM) 可降低 TBK1 敲除及匹配的野生型 MEFs 中的 LC3-II 水平[1]。
    MRT68921 dihydrochloride (24 h) 在癌细胞中表现出细胞毒性，其 IC50 值范围为 1.76-8.91 μM[2]。
    MRT68921 dihydrochloride (0-10 μM, 8-24 h) 可诱导 NCI-H460 和 MNK45 细胞中活性氧 (ROS) 的产生和凋亡[2]。
    MRT68921 dihydrochloride (0-5 μM, 8h) 可抑制 U251 和 MNK45 细胞中的 NUAK1/MYPT1/Gsk3β 及自噬相关信号通路[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    MRT68921 dihydrochloride 相关抗体:

    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.
    体内研究
    (In Vivo)

    MRT68921 dihydrochloride (10-40 mg/kg，皮下注射，每日 1 次，共 7 次) 在 NCI-H460 肿瘤小鼠模型中可抑制肿瘤生长[2]。
    MRT68921 dihydrochloride (20 mg/kg，皮下注射，每两天 1 次，共 7 次) 在 MNK45 肿瘤小鼠模型中可抑制肿瘤生长[2]。
    MRT68921 dihydrochloride (20 mg/kg，腹腔注射，每日 1 次，共 7 次) 可减少 4T1 肿瘤小鼠模型的肺转移结节数量[2]。

    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.
    分子量

    507.50

    Formula

    C25H36Cl2N6O
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 20.83 mg/mL (41.04 mM; 超声助溶 (<60°C))

    DMSO 中的溶解度 : 8.33 mg/mL (16.41 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9704 mL 9.8522 mL 19.7044 mL
    5 mM 0.3941 mL 1.9704 mL 3.9409 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.67%

    COA (284 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献

    MRT68921 dihydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.9704 mL 9.8522 mL 19.7044 mL 49.2611 mL
    5 mM 0.3941 mL 1.9704 mL 3.9409 mL 9.8522 mL
    10 mM 0.1970 mL 0.9852 mL 1.9704 mL 4.9261 mL
    15 mM 0.1314 mL 0.6568 mL 1.3136 mL 3.2841 mL
    H2O 20 mM 0.0985 mL 0.4926 mL 0.9852 mL 2.4631 mL
    25 mM 0.0788 mL 0.3941 mL 0.7882 mL 1.9704 mL
    30 mM 0.0657 mL 0.3284 mL 0.6568 mL 1.6420 mL
    40 mM 0.0493 mL 0.2463 mL 0.4926 mL 1.2315 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    MRT689212080306-21-2MRT 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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