EPZ 015666
Chemical Name: N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Background References
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Structure and property guided design in the identification of PRMT5 tool compound EPZ015666.
Duncan et al.
ACS Med.Chem.Lett., 2015;7:162 -
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Chan-Penebre et al.
Nat.Chem.Biol., 2015;11:432
Product Datasheets
Citation for EPZ 015666
The citations listed below are publications that use Tocris products. Selected citations for EPZ 015666 include:
1 Citation: Showing 1 - 1
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Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation.
Authors: Omar Et al.
Cancer Cell 2019;36:194-209.e9
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