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GLS1 Inhibitor-3

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GLS1 Inhibitor-3 

GLS1 Inhibitor-3 (compound C147) 是一种有效的 GLS1 抑制剂，IC50 为 27.98 nM。GLS1 Inhibitor-3 具有抗增殖活性。

GLS1 Inhibitor-3

GLS1 Inhibitor-3 Chemical Structure

CAS No. : 2435781-94-3

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生物活性

GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity[1].

IC50 & Target

IC50: 27.98 nM (GLS1)[1]
分子量

596.71

Formula

C30H32N10O2S
CAS 号

2435781-94-3
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.
参考文献

  • [1]. Xu X, et al. Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles. Eur J Med Chem. 2022 Jun 5;236:114337.

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GLS1 Inhibitor-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GLS1 Inhibitor-4 

GLS1 Inhibitor-4 (compound 41e) 是一种有效的 GLS1 抑制剂，IC50 为 11.86 nM。GLS1 Inhibitor-4 显示出抗增殖活性、良好的代谢稳定性和强大的 GLS1 结合亲和力。GLS1 Inhibitor-4 阻断谷氨酰胺代谢并诱导 ROS 的产生。GLS1 Inhibitor-4 可诱导细胞凋亡 (apoptosis)并显示出抗肿瘤活性。

GLS1 Inhibitor-4

GLS1 Inhibitor-4 Chemical Structure

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生物活性

GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity[1].

IC50 & Target

IC50: 11.86 nM (GLS1)[1]
体外研究
(In Vitro)

GLS1 Inhibitor-4 (compound 41e) shows antiproliferative activity with IC50s of 0.051, 0.37, 0.32, 1.34 µM for HCT116 and MDA-MB-436, CT26, H22 cells, respectively[1].
GLS1 Inhibitor-4 shows good plasma and liver microsomal stability with 96% stability in Human plasma[1].
GLS1 Inhibitor-4 shows robust binding affinity with GLS1 protein, the dissociation constants (Kd) of 52 nM[1].
GLS1 Inhibitor-4 (0.1, 0.5, 1 µM) inhibits the colony formation of HCT116 cells in a dose-dependent manner[1].
GLS1 Inhibitor-4 (100, 300 nM, 12 h) reduces the concentration of a number of key metabolites downstream of glutamate within 12 h[1].
GLS1 Inhibitor-4 (30, 50, 200 nM; 6 h) increases the ROS levels in a dose-dependent manner in HCT116 cells[1].
GLS1 Inhibitor-4 (1 mmol/L; 12 h) significantly decreases the ATP production basal and maximal OCRs (oxygen consumption rates) after 12 h, suppresses the aerobic glycolysis in HCT116 cancer cells[1].
GLS1 Inhibitor-4 (30, 50, 200 nM; 24 h) induces apoptosis in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 30, 50, 200 nM
Incubation Time: 24 h
Result: Induced approximately 28% and 95% more apoptotic cells at concentrations of 50 and 200 nM, respectively. And upregulated the expression of apoptotic protein cleaved PARP in a dose-dependent manner.

体内研究
(In Vivo)

GLS1 Inhibitor-4 (50, 100 mg/kg; i.p.; twice a day for 21 consecutive days) shows antitumor activity in a dose-dependent manne[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old BALB/c SPF nude mice (HCT116 tumor nude mouse xenograft model)[1]
Dosage: 50, 100 mg/kg
Administration: I.p.; twice a day for 21 consecutive days
Result: Inhibited the tumor growth at a dose-dependent manne with the tumor growth inhibition (TGI) values of 35.5% at 50 mg/kg and 47.5% at 100 mg/kg, respectively.

分子量

668.72

Formula

C29H27F3N10O2S2
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.
参考文献

  • [1]. Xu X, et al. Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles. Eur J Med Chem. 2022 Jun 5;236:114337.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GLS-1-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GLS-1-IN-1 

GLS-1-IN-1 (compound 1d) 是一种 GLS-1 抑制剂。GLS-1-IN-1 对 Hep G2、MCF 7 和 MCF 10A 细胞有抑制作用。

GLS-1-IN-1

GLS-1-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells[1].

分子量

460.57

Formula

C26H25FN4OS
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.
参考文献

  • [1]. Carbone D, et al. Metabolomics-assisted discovery of a new anticancer GLS-1 inhibitor chemotype from a nortopsentin-inspired library: From phenotype screening to target identification. Eur J Med Chem. 2022;234:114233.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GLS-1-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GLS-1-IN-1 

GLS-1-IN-1 (compound 1d) 是一种 GLS-1 抑制剂。GLS-1-IN-1 对 Hep G2、MCF 7 和 MCF 10A 细胞有抑制作用。

GLS-1-IN-1

GLS-1-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells[1].

分子量

460.57

Formula

C26H25FN4OS
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.
参考文献

  • [1]. Carbone D, et al. Metabolomics-assisted discovery of a new anticancer GLS-1 inhibitor chemotype from a nortopsentin-inspired library: From phenotype screening to target identification. Eur J Med Chem. 2022;234:114233.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GLS-1-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GLS-1-IN-1 

GLS-1-IN-1 (compound 1d) 是一种 GLS-1 抑制剂。GLS-1-IN-1 对 Hep G2、MCF 7 和 MCF 10A 细胞有抑制作用。

GLS-1-IN-1

GLS-1-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells[1].

分子量

460.57

Formula

C26H25FN4OS
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.
参考文献

  • [1]. Carbone D, et al. Metabolomics-assisted discovery of a new anticancer GLS-1 inhibitor chemotype from a nortopsentin-inspired library: From phenotype screening to target identification. Eur J Med Chem. 2022;234:114233.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务