2. Metabolic Enzyme/Protease Apoptosis
  3. Glutaminase Apoptosis
  4. LWG-301

LWG-301 是 Glutaminase 1 (GLS1) 的变构抑制剂 (IC50=7 nM)。LWG-301 显著阻断谷氨酰胺代谢，增加细胞内 ROS，从而诱导细胞凋亡 (apoptosis)。LWG-301 在 HCT116 异种移植模型中表现出中等的抗肿瘤作用。

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LWG-301 Chemical Structure

LWG-301 Chemical Structure

CAS No. : 3038480-88-2

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LWG-301 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model[1].

体外研究
(In Vitro)

LWG-301 (compound 41a) inhibits HCT116 cancer cells growth with an IC50 value of 61 nM[1].
LWG-301 has great metabolic stability in human liver microsomes with T1/2=108 min, CL=32 μL/min/mg[1].
LWG-301 (10 μM; 6 h) interacts with GLS1 protein in a dose- and time-dependent manner[1].
LWG-301 (0.03-3 μM; 14 d) inhibits the colony formation of HCT116 cells in a concentration-dependent manner[1].
LWG-301 (0.2 μM, 1 μM, 5 μM; 24 h) blocks the metabolism of glutamine thus results a decrease of glutamate, glutathione, and fumaric acid[1].
LWG-301 (1-10 μM; 24 h) induces ROS production and (0.1-10 μM; 24 h) induces apoptosis in HCT116 cells[1].

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

LWG-301 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.001, 0.01, 0.1, 1, and 10 μM
Incubation Time: 10, 30, 60, 180, 240 min
Result: Showed the interaction with GLS1 in a dose- and time-dependent manner.

Immunofluorescence[1]

Cell Line: HCT116 cells
Concentration: 1, 5, and 10 μM
Incubation Time: 6 hours
Result: Induced ROS production in HCT116 cells.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.1, 0.3, 1, 3, and 10 μM
Incubation Time: 24 hours
Result: Induced apoptosis in HCT116 cells
体内研究
(In Vivo)

LWG-301 (compound 41a) (100 mg/kg; i.p.; once daily for 20 d) shows anti-tumor activity without in HCT116 xenograft tumor model in mice[1].

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

Animal Model: HCT116 tumor-bearing nude mice[1]
Dosage: 100 mg/kg;
Administration: Intraperitoneal injection; once a day for 20 days;
Result: Reduced tumor growth, resulting in 38.9% tumor growth inhibition.
Showed little toxicity on main organ.
分子量

566.72

Formula

C28H38N8O3S
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

LWG-301 相关分类

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  • 稀释计算器

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  • 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:

LWG-3013038480-88-2LWG301LWG 301GlutaminaseApoptosisInhibitorinhibitorinhibit

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