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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
Technical Data for EPZ 015666
|Storage||Store at -20°C|
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|
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.
|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|
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
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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
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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
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.