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 hydrochloride

MRT68921 hydrochloride 是一种强效的 NUAK1/ULK1 双重抑制剂。MRT68921 hydrochloride 抑制 ULK1 和 ULK2 的 IC50 值分别为 2.9 nM 和 1.1 nM。MRT68921 hydrochloride 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 hydrochloride 能够抑制细胞增殖，诱导活性氧 (ROS) 的产生和细胞凋亡 (apoptosis)。MRT68921 hydrochloride 可用于癌症研究，如乳腺癌。

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MRT68921 hydrochloride

MRT68921 hydrochloride Chemical Structure

CAS No. : 2070014-87-6

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MRT68921 hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of MRT68921 hydrochloride:

MRT68921 hydrochloride 相关抗体

Top Publications Citing Use of Products

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

MRT68921 hydrochloride (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 hydrochloride (1 μM) 可降低 TBK1 敲除及匹配的野生型 MEFs 中的 LC3-II 水平[1]。
MRT68921 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride 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 hydrochloride (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 hydrochloride (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 hydrochloride (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

471.04

Formula

C25H35ClN6O
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MRT68921 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

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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