5.06069
3-Deazaneplanocin A hydrochloride
InSolution, ≥98%, 25 mM aqueous solution, EZH2 Inhibitor
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别名:
InSolution EZH2 Inhibitor, DZNep, 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
经验公式（希尔记法）:
C12H14N4O3 · 3HCl · 2H2O
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质量水平
检测方案
≥98% (HPLC)
形式
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
avoid repeated freeze/thaw cycles
protect from light
储存温度
−70°C
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
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.
生化/生理作用
Cell permeable: yes
Primary Target
EZH2
EZH2
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
外形
A 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H₂O.
重悬
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 monthst at -20°C.
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.
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
12 - Non Combustible Liquids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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