GSK-2816126

inhibits EZH2 methyltransferase; structure in first source

Also Known As:

1-((2S)-2-Butanyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl)-3-methyl-6-(6-(1-piperazinyl)-3-pyridinyl)-1H-indole-4-carboxamide; 1H-Indole-4-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-3-methyl-1-((1S)-1-methylpropyl)-6-(6-(1-piperazinyl)-3-pyridinyl)-; GSK126; GSK2816126

Networked: 65 relevant articles (5 outcomes, 8 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyridines: 88
    - Pyridones: 14
      - GSK-2816126: 65
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Indoles: 200
      - GSK-2816126: 65

Experts

1.	van Lohuizen, Maarten: 4 articles (01/2022 - 10/2016)
2.	Pan, Jingxuan: 3 articles (01/2020 - 01/2017)
3.	Zhu, Feng: 3 articles (01/2018 - 01/2016)
4.	Gong, Yueqing: 2 articles (03/2022 - 01/2022)
5.	Guo, Zhengyang: 2 articles (03/2022 - 01/2022)
6.	Huang, Jiaqi: 2 articles (03/2022 - 01/2022)
7.	Li, Chen: 2 articles (03/2022 - 01/2022)
8.	Ma, Xiaojuan: 2 articles (03/2022 - 01/2022)
9.	Wang, Yan: 2 articles (03/2022 - 01/2022)
10.	Xue, Lixiang: 2 articles (03/2022 - 01/2022)

Related Diseases

1.	Neoplasms (Cancer) 03/01/2022 - "In this study, we utilized the multiple cancer cell lines, which are less sensitive to the EZH2 inhibitor GSK126, combining animal model and clinical data to investigate the underlying mechanism. " 01/01/2022 - "Moreover, our study provided new insight for better understanding of the role of two kinds of EZH2i: EPZ6438 and GSK126, which may pave the way in treating CRC by targeting cancer cells and immune cells via this epigenetic approach in the future." 01/01/2016 - "GSK126, a specific inhibitor of EZH2, is undergoing phase I trials for hypermethylation-related cancers. " 01/01/2023 - "In vivo, ZLD-2 exhibited antitumor activity in a BxPC-3 mouse xenograft model, whereas GSK126 promoted tumor growth. " 12/01/2022 - "Administration of the EZH2 inhibitor GSK126 decreased CCA tumor burden in mice. "
2.	Prostatic Neoplasms (Prostate Cancer) 01/01/2016 - "GSK126 may be used as a potential anti-prostate cancer dug in clinic." 01/01/2016 - "Conclusion: GSK126 can significantly inhibit cell migration and invasion in prostate cancer PC-3 and DU145 cells, which may be resulted from its effect on epithelial-mesenchymal transition. " 01/01/2016 - "Methods: Prostate cancer PC-3 and DU145 cells were treated with GSK126 at different doses. " 01/01/2016 - "Objective: To investigate the effect of a novel EZH2 inhibitor GSK126 on cell growth, apoptosis and migration of prostate cancer cells. " 01/01/2016 - "[Effect of a novel EZH2 inhibitor GSK126 on prostate cancer cells]."
3.	Glioma (Gliomas) 10/01/2023 - "Furthermore, we demonstrated the effect of the EZH2-specific inhibitor GSK126 on GSCs; these results not only corroborate our hypothesis, but also provide a potential novel treatment approach for glioma."
4.	Atherosclerosis 08/01/2021 - "In conclusion, the present study provided new insights into the molecular mechanism behind the action of GSK126 and suggested its therapeutic potential for the treatment of atherosclerosis." 08/01/2021 - "These results indicated that the GSK126 has the ability to attenuate the progression of atherosclerosis by reducing macrophage foam cell formation and monocyte adhesion in cell and mouse models. " 08/01/2021 - "The present study aimed to determine the effects of the EZH2 inhibitor, GSK126, on the suppression and regression of atherosclerosis in apolipoprotein E-deficient mouse models. " 08/01/2021 - "Pharmacological inhibition of EZH2 by GSK126 decreases atherosclerosis by modulating foam cell formation and monocyte adhesion in apolipoprotein E-deficient mice." 08/01/2021 - "In vitro, it was found that pharmacological inhibition of EZH2 by GSK126 markedly reduced lipid transportation and monocyte adhesion during atherogenesis, predominantly through increasing the expression levels of ATP-binding cassette transporter A1 and suppressing vascular cell adhesion molecule 1 in human THP-1 cells. "
5.	Diffuse Large B-Cell Lymphoma (Lymphoma, Large Cell, Diffuse) 09/07/2020 - "In the current study, a combination of pomalidomide and GSK126 synergistically inhibited the growth of EZH2 gain-of-function mutant Diffuse large B-cell lymphoma (DLBCL) cells. " 09/07/2020 - "Combination Treatment with GSK126 and Pomalidomide Induces B-Cell Differentiation in EZH2 Gain-of-Function Mutant Diffuse Large B-Cell Lymphoma."

Related Drugs and Biologics

1.	tazemetostat
2.	Neutralizing Antibodies
3.	Metformin (Glucophage)
4.	Fluorouracil (Carac)
5.	Bezafibrate
6.	Differentiation Antigens
7.	Gemcitabine
8.	Enhancer of Zeste Homolog 2 Protein
9.	Apolipoproteins
10.	pomalidomide

Related Therapies and Procedures

1.	Therapeutics
2.	Castration
3.	Ovariectomy (Oophorectomy)
4.	Injections
5.	Immunotherapy