Product Details
| Product Name:
GSK591 |
CAS No.:
1616391-87-7 |
| Purity:
99.77% |
Supply Ability:
10g |
| Release date:
2025/07/25 |
Product Introduction
Bioactivity
| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (157.7 mM), Sonication is recommended.
|
| Keywords | PRMT5 | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | GSK-591 | GSK591 | GSK-3203591 | GSK 591 | GSK 3203591 | EPZ-015866 | EPZ 015866 |
| Inhibitors Related | MAK-683 hydrochloride | BIX-01294 trihydrochloride | ORIC-944 | Tazemetostat | Piribedil | XY1 | MAK683 | EPZ015666 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Histone Modification Compound Library | Reprogramming Compound Library | Methylation Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Chromatin Modification Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States