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
Reviews
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
water 45.34 100
DMSO 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.

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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References

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


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Citations for GSK 591 dihydrochloride

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