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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 |
|---|
| EPZ005687
EPZ005687 is a potent, selective EZH2 inhibitor,Ki The value is 24 nM, which is 50 times more selective than EZH1 and 500 times more selective than 15 other methyltransferases. |
| GSK343
GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. |
| UNC1999
UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. |
| CPI-169 racemate
CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. |
| 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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