Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 41.00 | |
2 mg | In stock | $ 56.00 | |
5 mg | In stock | $ 102.00 | |
10 mg | In stock | $ 147.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 513.00 | |
100 mg | In stock | $ 747.00 | |
500 mg | In stock | $ 1,560.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 108.00 |
Description | GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM). |
Targets&IC50 | PRMT5:11 nM |
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]. |
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. |
Synonyms | GSK3203591, EPZ015866 |
Molecular Weight | 380.48 |
Formula | C22H28N4O2 |
CAS No. | 1616391-87-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.3 mg/mL (100 mM)
You can also refer to dose conversion for different animals. More
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GSK591 1616391-87-7 Chromatin/Epigenetic Histone Methyltransferase EPZ 015866 GSK 591 EPZ-015866 Inhibitor inhibit GSK-3203591 GSK3203591 GSK 3203591 EPZ015866 GSK-591 inhibitor