EPZ015666 CAS:170355-78-9

背景资料

Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression.{18398,18480} PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas.{28582} Moreover, suppression of PRMT5 expression induces lymphoma cell death.{28581} EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).{28891} It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.{28891}

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品牌介绍

Cayman Chemical向全球科学工作者提供多研究领域的生化、免疫试剂和分析试剂盒，其产品被广泛应用于肿瘤、氧化氮、神经学、凋亡、氧化性损伤、内分泌学等不同研究领域.Cayman Chemical可提供用于检测的特色试剂盒，如：类花生酸类物质、游离的生物标志、环核苷、激素及氧化氮等；也提供多种高质量试剂，包括：类花生酸类物质、氧化氮试剂及许多相关脂质、脂肪酸、酶和抗体.作为Cayman Chemical在中国的区域总代理，艾美捷科技有限公司将为中国客户提供最全面的Cayman Chemical产品以及客户订制化服务.

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