2. Metabolic Enzyme/Protease Apoptosis
  3. Glutaminase Apoptosis
  4. 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。

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GLS1 Inhibitor-4 Chemical Structure

GLS1 Inhibitor-4 Chemical Structure

CAS No. : 2768599-97-7

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GLS1 Inhibitor-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CT26 IC50
0.32 μM
Compound: 41e
Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 35428013]
H22 IC50
10.84 μM
Compound: 41e
Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 35428013]
HCT-116 IC50
0.051 μM
Compound: 41e
Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 35428013]
MDA-MB-436 IC50
0.37 μM
Compound: 41e
Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 35428013]
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].

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

GLS1 Inhibitor-4 相关抗体:

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].

MCE 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
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

GLS1 Inhibitor-4 相关分类

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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:

GLS1 Inhibitor-42768599-97-7GlutaminaseApoptosisantitumorantiproliferativemetabolic stabilityglutamine metabolismROSapoptosisBALB/c SPF nude miceHCT116 cellsInhibitorinhibitorinhibit

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