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GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.
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Source | Oncotarget (2017). Figure 2. GSK126 |
| Method | Clonogenicity | |
| Cell Lines | multiple myeloma cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | The results showed that after exposure to GSK126 for 24 h, the colonyformation ability of MM cells were significantly reduced with IC50 < 10 μM |
| Cell Experiment | |
|---|---|
| Cell lines | EZH2 wildtype or mutant B-cell lymphoma cell lines |
| Preparation method | Cell proliferation assay. The optimal cell seeding was determined empirically for all cell lines by examining the growth of a wide range of seeding densities in a 384-well format to identify conditions that permitted proliferation for 6 days. Cells were then plated at the optimal seeding density 24 h before treatment (in duplicate) with a 20-point twofold dilution series of GSK126 or 0.15% DMSO. Plates were incubated for 6 days at 37℃ in 5% CO2. Cells were then lysed with CellTiter-Glo (CTG) (Promega) and chemiluminescent signal was detected with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells was harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values obtained after the 6 day treatment were expressed as a percent of the T0 value and plotted against compound concentration. Data were fit with a four-parameter equation to generate a concentration response curve and the concentration of GSK126 required to inhibit 50% of growth (growth IC50) was determined. |
| Concentrations | 0~100µM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | Pfeiffer or KARPAS-422 cells tumour xenograft in mice |
| Formulation | 20% captisol adjusted to pH 4–4.5 with 1 N acetic acid. |
| Dosages | 0.2 ml per 20 g body weight |
| Administration | intraperitoneally |
| Molecular Weight | 526.67 |
| Formula | C31H38N6O2 |
| CAS Number | 1346574-57-9 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related EZH2 Products |
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Tulmimetostat is an orally active dual EZH1/EZH2 protein inhibitor with antitumor activity for use in a variety of solid tumor studies. |
| PF-06821497
PF-06821497 is a selective and orally active Zeste Homolog 2 (EZH2) inhibitor with powerful tumor growth inhibition. |
| CPI-1205
CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. |
| Valemetostat
Valemetostat (DS-3201, DS-3201b) is a first-in-class dual inhibitor targeting EZH1 and EZH2. It can be used in the study of adult T-cell leukemia/lymphoma. |
| MS1943
MS1943 is a pioneering oral bioactive selective EZH2 inhibitor with an IC50 of 120 nM. MS1943 significantly reduced EZH2 protein levels in many triple negative breast and other cancers and non-cancer lines. MS1943 effectively blocked the proliferation of multiple triple negative breast cancers and other cancer lines. |
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