EPZ015666 is a selective and potent (IC50 = 22nM) inhibitor of arginine methyltransferase 5 (PRMT5).1,2 PRMT5 inhibition with EPZ015666 potently suppressed in vivo glioblastoma tumors3 and significantly inhibited the growth of multiple myeloma cell lines4.
1) 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
2) Duncan et al. (2015), Structure and Property Guided Design in the Identification of PRMT5 Toll Compound EPZ015666; ACS Med. Chem. Lett. 7 162
3) Braun et al. (2017), Coordinated Splicing of Regulatory Detained Introns within Oncogenic Transcripts Creates an Exploitable Vulnerability in Malignant Glioma; Cancer Cell 32 411
4) Gulia et al. (2018), Protein arginine methyltransferase 5 has prognostic relevance and is a druggable target in multiple myeloma; Leukemia 32 996