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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-ZLD1039
ZLD1039

Chemical Structure : ZLD1039

CAS No.: 1826865-46-6

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ZLD1039 (ZLD 1039, ZLD-1039)

货号: PC-72288Not For Human Use, Lab Use Only.

ZLD1039 (ZLD 1039) is a potent, highly selective, and orally bioavailable small molecule inhibitor of EZH2 with IC50 of 5.6, 15, 4.0 nM against EZH2 WT, Y641F, and A677G mutations respectively.

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10 mg ￥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ZLD1039 (ZLD 1039) is a potent, highly selective, and orally bioavailable small molecule inhibitor of EZH2 with IC50 of 5.6, 15, 4.0 nM against EZH2 WT, Y641F, and A677G mutations respectively.
ZLD1039 displays high selectivity against a panel of HMTs, including EZH1, SETD7, SUV39H1, G9a, DOT1L, SUV39H2, SMYD2, PRDM9, SETD8, NSD3 and MLL1.
ZLD1039 inhibited the H3K27me3 and H3K27me2 levels in MCF-7 (IC50=0.29 uM) and MDA-MB-231 cells in a dose-dependent manner.
ZLD1039 showed antiproliferative activities against breast cancer cells in vitro (MCF-7 cell GI50=0.0.99 uM), induced G0/G1 phase arrest, apoptosis and transcription activation. ZLD1039 demonstrated anti-tumor and anti-tumor metastasis activity in breast xenograft animal models.

物理化学性质&存储条件

分子量 612.819
分子式 C36H48N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(Ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methyl-N-((1-methyl-3-oxo-2,3,5,6,7,8-hexahydroisoquinolin-4-yl)methyl)-5-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)benzamide

参考文献

1. Song X, et al. Sci Rep. 2016 Feb 12;6:20864.

2. Song X, et al. Sci Rep. 2016 Apr 29;6:24893.

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