| Name | GSK591 |
| Description | GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM). |
| Kinase Assay | Selectivity profiling experiments: The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or GSK2141795) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide. |
| In vitro | In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases[1][2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (157.7 mM)
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| Keywords | EPZ 015866 | GSK 591 | GSK591 | EPZ-015866 | Inhibitor | inhibit | GSK-3203591 | Histone Methyltransferase | GSK 3203591 | GSK-591 |
| Inhibitors Related | BIX-01294 trihydrochloride | Tazemetostat | Piribedil | XY1 | UNC 0631 | GSK126 | MAK683 | EZM 2302 | EPZ015666 | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Histone Modification Compound Library | Methylation Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library |
United States
