Chemical Name: N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
Biological ActivityPotent 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.
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.
Structure and property guided design in the identification of PRMT5 tool compound EPZ015666.
Duncan et al.
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Chan-Penebre et al.
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