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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.
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.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
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: