GSK 591 dihydrochloride

Name: GSK 591 dihydrochloride
Brand: Tocris Bioscience
SKU: 5777

Tocris Bioscience, part of Bio-Techne | Catalog # 5777

COA / SDS

Potent and selective PRMT5 inhibitor

Key Product Details

Description:	Potent and selective PRMT5 inhibitor
Alternative Names:	EPZ015866,GSK 3203591
Chemical Name:	2-(Cyclobutylamino)-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydropropyl]-4-pyridinecarboxamide dihydrochloride
Purity:	≥97% (HPLC)
Molecular Weight:	453.41

View Full Technical Details for GSK 591 dihydrochloride

Technical Data
Citations

Biological Activity for GSK 591 dihydrochloride

GSK 591 dihydrochloride is a potent and selective PRMT5 inhibitor (IC₅₀ = 4 nM). Selective for PRMT5 over a panel of other PRMTs and lysine methyltransferases. Inhibits proliferation of mantle cell lymphoma (MCL) in vitro.

To request the negative control for GSK 591, please fill out the SGC 2096 request form on the SGC website.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK591 probe summary on the SGC website.

Compound Libraries for GSK 591 dihydrochloride

GSK 591 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK591 is reviewed on the Chemical Probes website.

Technical Data for GSK 591 dihydrochloride

M. Wt	453.41
Formula	C₂₂H₂₈N₄O₂.2HCl
Storage	Desiccate at RT
Purity	≥97% (HPLC)
CAS Number	2320953-89-5
PubChem ID	124201849
InChi Key	CDKUMVXFXBTOBE-FJSYBICCSA-N
Smiles	O[C@@H](CNC(C1=CC=NC(NC2CCC2)=C1)=O)CN3CC4=CC=CC=C4CC3.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 591 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	45.34	100
	DMSO	45.34	100

Preparing Stock Solutions for GSK 591 dihydrochloride

The following data is based on the product molecular weight 453.41.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.21 mL	11.03 mL	22.06 mL
5 mM	0.44 mL	2.21 mL	4.41 mL
10 mM	0.22 mL	1.10 mL	2.21 mL
50 mM	0.04 mL	0.22 mL	0.44 mL

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Reconstitution Calculator

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References for GSK 591 dihydrochloride

References are publications that support the biological activity of the product.

Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
Duncan Structure and property guided design in the identification of PRMT5 tool compound EPZ015666. ACS.Med.Chem.Lett. 2015 PMID: 26985292