GSK 591 dihydrochloride

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Cat.No. 5777 - GSK 591 dihydrochloride | C22H28N4O2.2HCl | CAS No. 1616391-87-7
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)
Datasheet
Citations
Literature

Biological Activity

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.

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

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

M. Wt 453.41
Formula C22H28N4O2.2HCl
Storage Desiccate at RT
Purity ≥97% (HPLC)
CAS Number 1616391-87-7
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 453.41. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Citations for GSK 591 dihydrochloride

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases

Pathways for GSK 591 dihydrochloride

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