生化/生理作用
Potent and selective SETD2 inhibitor with anti-cancer efficacy.
EPZ-719 is a potent and selective SETD2 inhibitor (Ki/IC50 = 3.3/8 nM), being > 8000-fold more selective towards SETD2 over 14 other histone methyltransferases, including the mono/di-H3K36 methylases SMYD2 and WHSC1/MMSET/NSD2. EPZ-719 downregulates cellular H3K36 trimethylation level (IC50 = 23 nM, A549 cells) and shows potent anti-proliferative activity against multiple myeloma cell lines (IC50 in 14 days = 25 nM/KMS34, 11 nM/KMS211) and good pharmacokinetic properties in mice.
EPZ-719 is a potent and selective SETD2 inhibitor (Ki/IC50 = 3.3/8 nM), being > 8000-fold more selective towards SETD2 over 14 other histone methyltransferases, including the mono/di-H3K36 methylases SMYD2 and WHSC1/MMSET/NSD2. EPZ-719 downregulates cellular H3K36 trimethylation level (IC50 = 23 nM, A549 cells) and shows potent anti-proliferative activity against multiple myeloma cell lines (IC50 in 14 days = 25 nM/KMS34, 11 nM/KMS211) and good pharmacokinetic properties in mice.
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持