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位置: 首页> 品牌> Sigma-Aldrich> InSolution EZH2 Inhibitor, DZNep-CAS 102052-95-9-Calbiochem

InSolution EZH2 Inhibitor, DZNep-CAS 102052-95-9-Calbiochem

品牌
Sigma-Aldrich
CAS
102052-95-9
货号
5.06069
规格纯度
A 25 mM (1 mg/98 μL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep in H2O.
价格
2004.27 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
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半岛bd体育手机客户端 名称:
102052-95-9
InSolution EZH2 Inhibitor, DZNep-CAS 102052-95-9-Calbiochem
3-Deazaneplanocin A, xHCl, yH 2O {x = 3 & y = 2}, (1 S,2 R,5 R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol, xHCl, yH 2O {x = 3 & y = 2}, NSC 617989
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable compound that is shown (at 1 ?M 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/G1phase (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
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外形

A 25 mM (1 mg/98 ?L) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H?O.

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.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C12H14N4O3· 3HCl · 2H2O
分子量 407.68

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 liquid
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
avoid repeated freeze/thaw cycles
protect from light
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

安全信息

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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