EPZ 015666

Pricing Availability   Qty
Description: Potent and selective PRMT5 inhibitor
Chemical Name: N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
Citations (1)
Literature (1)

Biological Activity for EPZ 015666

EPZ 015666 is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50 = 22 nM, Ki = 5 nM). Displays selectivity for PRMT5 over a panel of 20 other protein methyltransferases. Exhibits dose-dependent antitumor effects in multiple mantle cell lymphoma (MCL) xenograft models. Orally bioavailable.

Compound Libraries for EPZ 015666

EPZ 015666 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for EPZ 015666

M. Wt 383.44
Formula C20H25N5O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1616391-65-1
PubChem ID 90241673
Smiles O[C@H](CN1CCC2=CC=CC=C2C1)CNC(C3=NC=NC(NC4COC4)=C3)=O

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 EPZ 015666

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.34 100
ethanol 19.17 50

Preparing Stock Solutions for EPZ 015666

The following data is based on the product molecular weight 383.44. 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 2.61 mL 13.04 mL 26.08 mL
5 mM 0.52 mL 2.61 mL 5.22 mL
10 mM 0.26 mL 1.3 mL 2.61 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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References for EPZ 015666

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

Chan-Penebre et al (2015) A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat.Chem.Biol. 11 432 PMID: 25915199

If you know of a relevant reference for EPZ 015666, please let us know.

View Related Products by Product Action

View all Protein Arginine Methyltransferase Inhibitors

Keywords: EPZ 015666, EPZ 015666 supplier, EPZ015666, GSK3235025, potent, selective, PRMT5, protein, arginine, methytransferase, 5, inhibitors, inhibits, Protein, Arginine, Methyltransferases, 6516, Tocris Bioscience

1 Citation for EPZ 015666

Citations are publications that use Tocris products. Selected citations for EPZ 015666 include:

Omar et al (2019) Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation. Cancer Cell 36 194-209.e9 PMID: 31408619

Do you know of a great paper that uses EPZ 015666 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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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.