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Gsk126

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GSK126 is a selective inhibitor of the histone methyltransferase EZH2. It functions by blocking the catalytic activity of EZH2, which is responsible for the methylation of histone H3 at lysine 27 (H3K27).

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Lab products found in correlation

Unc0638, by Merck Group (2 mentions) Dznep, by Cayman Chemical (1 mentions) 3 deazaneplanocin a, by Cayman Chemical (1 mentions) Anti cd3 cd28 antibodies, by Miltenyi Biotec (1 mentions) Cd4 t cell isolation kit, by Miltenyi Biotec (1 mentions) Fetal bovine serum (fbs), by Thermo Fisher Scientific (1 mentions) Ficoll paque, by GE Healthcare (1 mentions) Rpmi 1640 medium, by Thermo Fisher Scientific (1 mentions) Phorbol myristate acetate (pma), by LC Laboratories (1 mentions) Tnf α, by R&D Systems (1 mentions) Ez pcr mycoplasma detection kit, by Sartorius (1 mentions) Unc0642, by Merck Group (1 mentions) Rneasy mini kit, by Qiagen (1 mentions) S2101, by Merck Group (1 mentions) Gsk2879552, by Chemietek (1 mentions) Epz 5676, by Chemietek (1 mentions) Sgc0946, by Merck Group (1 mentions) Gsk j1, by Merck Group (1 mentions) Carfilzomib, by Selleck Chemicals (1 mentions) Bortezomib, by Selleck Chemicals (1 mentions)

5 protocols using gsk126

1

Cell culture and treatment protocol

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Jurkat, Molt4, CCRF-CEM, SupT1 and U1 cells were maintained in RPMI1640 medium (GIBCO) with 10% fetal bovine serum (FBS, GIBCO), and antibiotics (GIBCO). For exogenous stimulation, the cells were treated with PMA (LC Laboratories), Ionomycin (CALBIOCHEM), or TNF-α (R&D systems). For inhibition of epigenetic factors, the cells were treated with the indicated concentrations of VPA (SIGMA), SAHA (Cayman), TSA (SIGMA), 3-deazaneplanocin A (DZNep, Cayman), or GSK126 (Chemie Tek). HEK293T, HEK293FT, and Hela/LTR-luciferase cells were maintained in DMEM with 10% FBS and antibiotics. Human peripheral blood mononuclear cells (PBMCs) were prepared from whole blood of healthy donors by density gradient centrifugation with Ficoll-Paque (GE healthcare). CD4+ T cells were purified by CD4+ T cell isolation kit (Miltenyi Biotec) and maintained in RPMI1640 with 10% of FBS. T cell activation was accomplished by treating the anti-CD3/CD28 antibodies (Miltenyi Biotec).
Matsuda Y., Kobayashi-Ishihara M., Fujikawa D., Ishida T., Watanabe T, & Yamagishi M. (2015). Epigenetic Heterogeneity in HIV-1 Latency Establishment. Scientific Reports, 5, 7701.
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2

Compound Preparation and Characterization

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TAS‐117, trans‐3‐amino‐1methyl‐3‐[4‐(3‐phenyl‐5H‐imidazo [1,2‐c]pyrido[3,4‐e][1,3]oxazin‐2‐yl)phenyl]‐cyclobutanol, was obtained from Taiho Pharmaceutical Co., Ltd. and diluted in DMSO to form a stock of 20 μmol/L. UNC1999 was produced at the Icahn School of Medicine at Mount Sinai25 and was diluted in DMSO to a stock of 10 mmol/L. GSK126 was purchased from CHEMIETEK and was diluted in DMSO to a stock of 20 mmol/L.
Rizk M., Rizq O., Oshima M., Nakajima‐Takagi Y., Koide S., Saraya A., Isshiki Y., Chiba T., Yamazaki S., Ma A., Jin J., Iwama A, & Mimura N. (2019). Akt inhibition synergizes with polycomb repressive complex 2 inhibition in the treatment of multiple myeloma. Cancer Science, 110(12), 3695-3707.
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3

Culturing and Authenticating Multiple Myeloma Cell Lines

Cited 1 time
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MM cell lines (RPMI-8226, MM.1S, KMS-11, KMS-12BM, KMS-12PE, and U-266) were obtained and cultured as described previously10 (link). Cell lines were authenticated using short tandem repeat analysis performed by JCRB (Tokyo, Japan) or BEX (Tokyo, Japan). They were also checked for mycoplasma with an EZ-PCR Mycoplasma Detection Kit (Biological Industries, Beit HaEmek, Israel) and were found to be negative. Total RNA was extracted using RNeasy Mini Kits (Qiagen, Hilden, Germany) according to the manufacturer’s instructions. EZH2 inhibitors (GSK126 and EPZ-6438) were purchased from Chemietek (Indianapolis, IN, USA). G9a inhibitors (UNC0638 and UNC0642) were from Sigma-Aldrich (St. Louis, MO, USA).
Ishiguro K., Kitajima H., Niinuma T., Maruyama R., Nishiyama N., Ohtani H., Sudo G., Toyota M., Sasaki H., Yamamoto E., Kai M., Nakase H, & Suzuki H. (2021). Dual EZH2 and G9a inhibition suppresses multiple myeloma cell proliferation by regulating the interferon signal and IRF4-MYC axis. Cell Death Discovery, 7, 7.
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4

Epigenetic Modulators: Inhibitor Evaluation

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The H3K4 methyltransferase LSD1 inhibitor S2101 was purchased from Merck Millipore (Burlington, MA, USA). The LSD1 inhibitor GSK2879552, H3K27 methyltransferase EZH2 inhibitor GSK126, and H3K79 methyltransferase DOT1L inhibitor EPZ-5676 were all purchased from Chemietek (Indianapolis, IN, USA). The H3K9 methyltransferase G9a inhibitor UNC0638, H3K27 demethylase JMJD3/UTX inhibitor GSKJ1, DOT1L inhibitor SGC0946, and MYC inhibitor 10058-F4 were all purchased from Sigma-Aldrich (St. Louis, MO, USA).
Ishiguro K., Kitajima H., Niinuma T., Ishida T., Maruyama R., Ikeda H., Hayashi T., Sasaki H., Wakasugi H., Nishiyama K., Shindo T., Yamamoto E., Kai M., Sasaki Y., Tokino T., Nakase H, & Suzuki H. (2019). DOT1L inhibition blocks multiple myeloma cell proliferation by suppressing IRF4-MYC signaling. Haematologica, 104(1), 155-165.
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5

Preparation and Dilution of Small Molecule Inhibitors

Cited 1 time
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UNC1999 was produced at Icahn School of Medicine at Mount Sinai (9 (link)) and was diluted in DMSO to a stock of 10 mmol/L for cell culture experiments. For in vivo experiments, UNC1999 was slowly dissolved in 5% DMSO in corn oil with vigorous vortex followed by rotation to achieve a homogenous suspension of 60 or 100 mg/mL. GSK126 was purchased from CHEMIETEK and was diluted in DMSO to a stock of 20 mmol/L. Bortezomib and carfilzomib for cell culture experiments were obtained from Selleck Chemicals and were diluted in DMSO to stocks of 100 μmol/L. Bortezomib was purchased from Janssen Pharmaceutical KK for in vivo experiments and was diluted in normal saline to a 1 mg/mL stock. MG132 was obtained from Cayman Chemical and was diluted in DMSO to a stock of 10 mmol/L.
Rizq O., Mimura N., Oshima M., Saraya A., Koide S., Kato Y., Aoyama K., Nakajima-Takagi Y., Wang C., Chiba T., Ma A., Jin J., Iseki T., Nakaseko C, & Iwama A. (2017). Dual Inhibition of EZH2 and EZH1 Sensitizes PRC2-Dependent Tumors to Proteasome Inhibition. Clinical cancer research : an official journal of the American Association for Cancer Research, 23(16), 4817-4830.
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