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InSolution EZH2 Inhibitor, DZNep-CAS 102052-95-9-Calbiochem
| 产品编号： | 4083549 |
| 规格： | A 25 mM (1 mg/98 μL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep in H2O. |
| CAS NO： | 102052-95-9 |
| 包装规格： | 1 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
102052-95-9
InSolution EZH2 Inhibitor, DZNep-CAS 102052-95-9-Calbiochem
3-Deazaneplanocin A, xHCl, yH2O {x = 3 & y = 2}, (1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol, xHCl, yH2O {x = 3 & y = 2}, NSC 617989
基本信息
| Empirical Formula【经验(实验)分子式】 | C12H14N4O3 · 3HCl · 2H2O |
| Molecular weight | 407.68 |
| General description【一般描述】 | 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. |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target EZH2 Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Physical form【外形】 | A 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H₂O. |
| Reconstitution【重悬】 | Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 monthst at -20°C. |
| Other Notes【其他说明】 | Sun, F., et al. 2009. Mol. Cancer Ther.8, 3191. Miranda, T.B., et al. 2009. Mol. Cancer Ther.8, 1579. Fiscus, W., et al. 2009. Blood13, 2733. Tan, J., et al. 2007. Genes Dev.21, 1050. Chiang, P.K., et al. 1992. J. Biol. Chem.267, 4988. Tseng, C.K., et al. 1989. J. Med. Chem.32, 1442. Glazer, R.I., et al. 1986. Biochem. Biophys. Res. Commun.135, 688. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze avoid repeated freeze/thaw cycles protect from light |
| storage temp.【储存温度】 | −70℃ |
| InChI | 1S/C12H14N4O3/c13-12-9-7(1-2-14-12)16(5-15-9)8-3-6(4-17)10(18)11(8)19/h1-3,5,8,10-11,17-19H,4H2,(H2,13,14)/t8-,10-,11+/m1/s1 |
| InChI key | OMKHWTRUYNAGFG-IEBDPFPHSA-N |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 12 - Non Combustible Liquids |
| WGK | WGK 2 |
