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Description: 3-deazaneplanocin A (known also as DZNep; NSC-617989), an adenosine analog, is a novel and competitive inhibitor of S-adenosylhomocysteine hydrolase and an EZH2 (histone methyltransferase ) inhibitor with anticancer activity. It inhibits S-adenosylhomocysteine hydrolase with a Ki of 50 pM in a cell-free assay. 3-deazaneplanocin A demostrates excellent antiproliferative activity and high in vivo antitumor efficacy. It disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma. DZNep is a promising therapeutic agent for ovarian cancer cells, with potential to inhibit proliferation, induce apoptosis and decrease migration.
References:Blood. 2009 Sep 24; 114(13):2733-43; J Med Chem. 1989 Jul; 32(7):1442-6.
Related CAS #: 120964-45-6 (HCl); 102052-95-9 (free base);
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