EPZ005687
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Cat.No：IE1470 Solarbio
CAS：1396772-26-1
Storage：Powder:-20℃，2 years
Purity：≥98%
Appearance：Off-white to yellow Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > EPZ005687
Product Information
| CAS | 1396772-26-1 |
| Name | EPZ005687 |
| Molecular Formula | C32H37N5O3 |
| Molecular Weight | 539.67 |
| Solubility | Soluble in DMSO ≥0.1mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:-20℃，2 years |
| MDL | MFCD25372029 |
| SMILES | O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6 |
| Target Point | Histone Methyltransferase（EZH2） |
| Passage | Epigenetics |
| Background | EPZ005687 is a potent and selective EZH2 inhibitor. |
| Biological Activity | EPZ005687 是一种有效的，选择性的 EZH2 抑制剂，Ki 值为 24 nM，对其选择性是对 EZH1 的 50 倍，对其他 15 种甲基转移酶的 500 倍。[1-2] |
| IC50 | Ki: 24nM(EZH2)[1] |
| In Vitro | EPZ005687显示PRC2酶活性的浓度依赖性抑制，IC 50值为54±5nM。 EPZ005687特异性抑制淋巴瘤细胞中的H3K27甲基化。 EPZ005687对携带EZH2Y641F的细胞系的增殖具有显著影响。 EPZ005687降低了突变体而非野生型EZH2淋巴瘤细胞的增殖[1]。 EPZ005687(0.5，1，5和10μM)以剂量依赖性方式诱导U937细胞的明显凋亡。 EPZ005687明显抑制U937细胞的增殖，但对NBMCD34 +细胞的增殖影响较小。 EPZ005687诱导G1期阻断并降低U937细胞中S期细胞的百分比。此外，EPZ005687在U937细胞中产生明显的H3K27甲基化缺失，但对NBMCD34 +细胞的H3K27甲基化几乎没有影响[2]。 |
| Cell Experiment | 对于细胞周期，将WSU-DLCL2细胞以1×10 5个细胞/ mL的密度接种在12孔板中。将细胞与EPZ005687以0.2μM，0.67μM，2μM和6μM一起孵育，总共2mL，历时10天。进行所有剩余的细胞周期分析。 |
| Kinase Experiment | EPZ005687的10点曲线使用在DMSO中的连续3倍稀释制备，从2.5mM开始(化合物的最终顶部浓度为50μM，DMSO为2％)。将1μL等分试样的抑制剂稀释系列点在384孔微量滴定板中。 100％抑制对照由1mM终浓度的产物抑制剂S-腺苷高半胱氨酸(SAH)组成。在1X测定缓冲液(20mM Bicine [pH 7.6]，0.002％吐温20，0.005％牛皮明胶中)将化合物与每孔40μL的5nM PRC2(50μL中的最终测定浓度为4nM)孵育30分钟。 0.5mM DTT)。每孔加入10μL底物混合物，其包含测定缓冲液3H-SAM，未标记的SAM和代表含有C-末端生物素的组蛋白H3残基21-44的肽(附加于C-末端酰胺封端的赖氨酸)以引发反应。将反应在室温下孵育90分钟，并用每孔10μL的600μM未标记的SAM淬灭，然后转移至384孔Flashplate并在30分钟后洗涤。 |
| Data Literature Source | [1]. Knutson SK，et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012;8(11):890-6. [2]. Tang SH，et al. Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis，proliferation and cell cycle of U937 cells and normal CD34 positive cells. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6 |
| Unit | Bottle |
| Specification | 5mg 10mg |
EPZ005687是一种有效的，选择性EZH2抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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