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merck millipore,默克密理博,252790,Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem
产品名称：Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem
产品型号：252790
merck millipore,默克密理博,252790,Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem
- 产品介绍
- merck millipore,默克密理博,252790,Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem
重要规格表
经验配方 CAS号 C₁₂H₁₄N₄O₃ • HCl • H₂O 120964-45-6 描述 概述 A cell-permeable compound that is shown (at 1 µM concentrations) to inhibit EZH2-mediated trimethylation of K27 on histone H3 and induces the expression of cell-cycle regulatory genes, p21 and p27, as well as the cell death regulator, FBXO32, in OCI-AML3 and HL-60 cells, whereby treatment with inhibitor increases p16 levels in the former, but not the latter of the two cultures. At concentrations between 200 nm and 2000 nM, this compound is found to dose-dependently deplete the expression of polycomb group proteins EZH2, SUZ12, and EED in cultured and primary AML cell extracts. At concentrations up to ≥ 1000 nM, DZNep dose-dependently increases the percentage of apoptotic cells up to > ~ 38%, with greater potency against OCI-AML3 than HL-60 cultures and inhibits colony growth up to > ~ 85% for both cell lines. In OCI-AML3 cultures, 1000 nM of treatment demonstrates a significant increase in the accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle. When co-treated with panobinostat (PS), 200 nM to 1000nM DZNep is shown to decrease cell viability in OCI-AML3 and HL-60 cultures more effectively than DZNep alone, in a dose-dependent manner. DZNep (1mg/kg, twice per week, i.p.) and PS significantly prolong the survival of mice implanted with HL-60 cells compared to treatment with either compound alone. DZNep is also a known S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitor. Also available as a 25 mM solution in H2O (Cat. No. 506069). 产品目录编号 252790 品牌系列 Calbiochem®
同义词 3-deazaneplanocin A, HCl; (1S,2R,5R)-5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol, HCl, HMTase Inhibitor X 参考 参考 Fiscus, W., et al. 2009. Blood 13, 2733. 产品信息 CAS号 120964-45-6 形式 Tan solid 配方 Supplied as a hydrochloride salt. Hill配方 C₁₂H₁₄N₄O₃ • HCl • H₂O 化学配方 C₁₂H₁₄N₄O₃ • HCl • H₂O 吸湿 Hygroscopic
结构配方图像 生物信息 纯度 ≥97% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 -20°C
避光 Protect from light
吸湿 Hygroscopic
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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