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GSK591

Catalog No. T6853 CAS 1616391-87-7

Synonyms: GSK3203591, EPZ015866

GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).

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GSK591, CAS 1616391-87-7

Pack Size	Availability	Price/USD
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

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Purity: 99.77%

Purity: 99.35%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.3 mg/mL (100 mM)

References and Literature

1. Elayne Chan-Penebre, et al. Nat Chem Biol. 2015, 11(6):432-437. 2. SGC. GSK591 A chemical probe for PRMT5. 3. Li W, He Y, Yang J, et al. Profiling PRMT methylome reveals roles of hnRNPA1 arginine methylation in RNA splicing and cell growth[J]. Nature Communications. 2021, 12(1): 1-20

Citations

1. Li W, He Y, Yang J, et al. Profiling PRMT methylome reveals roles of hnRNPA1 arginine methylation in RNA splicing and cell growth. Nature Communications. 2021, 12(1): 1-20

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Stem Cell Differentiation Compound Library Chromatin Modification Compound Library Target-Focused Phenotypic Screening Library Anti-COVID-19 Compound Library Anti-Aging Compound Library Histone Modification Compound Library Reprogramming Compound Library Methylation Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

CCI-007 BIX-01294 SETDB1-TTD-IN-1 SGC-iMLLT AMI-1 PRMT5-IN-25 MI-2-2 GSK467

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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