GSK 591 dihydrochloride

Pricing Availability   Qty
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)
Literature (1)

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.

External Portal Information for GSK 591 dihydrochloride 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.

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.

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
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 Data for GSK 591 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 1.1 mL 2.21 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets for GSK 591 dihydrochloride

References for GSK 591 dihydrochloride

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

Duncan et al (2015) Structure and property guided design in the identification of PRMT5 tool compound EPZ015666. ACS.Med.Chem.Lett. 7 162 PMID: 26985292

Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761

If you know of a relevant reference for GSK 591 dihydrochloride, please let us know.

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Keywords: GSK 591 dihydrochloride, GSK 591 dihydrochloride supplier, GSK591, dihydrochloride, protein, arginine, methyltransferases, inhibitors, inhibits, potent, selective, PRMT5, 1616391-87-7, Structural, Genomics, Consortium, SGC, GSK3203591, EPZ015866, GSK, 3203591, Protein, Arginine, Methyltransferases, 5777, Tocris Bioscience

Citations for GSK 591 dihydrochloride

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Literature in this Area

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Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.