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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
- CAS号：
2089148-72-9
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10 mM * 1 mL///1 mg
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A-395
CAS No. : 2089148-72-9
MCE 国际站：A-395
产品活性：A-395 是一种 polycomb 抑制复合物 2 (polycomb repressive complex 2; PRC2) 蛋白质-蛋白质相互作用的拮抗剂，抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12) 的 IC50 值为 18 nM。
研究领域：Epigenetics
作用靶点：Histone Methyltransferase
In Vitro: The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC50 of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3, with IC50 values of 390 nM and 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors.
In Vivo: The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC50 of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3, with IC50 values of 390 nM and 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors.
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文献和实验Clone information and RNAi Feeding Protocol
), which is a modified version of Bluescript with a T7 promoter on each side of the MCS driving transcription of each DNA strand (Nature, 395, 854). Information about the L4440 vector (including sequence information) can be found at http://www.ciwemb.edu. PCR fragments
1986;8(suppl 9):S1-S10 13 .Carafoli E Intracellular calcium homeostasis.Ann Rev Biochem 1987;56:395-433 14.Brown JH et al.Phosphoinositide-generated second messengers in cardiac signal transduction.Trends in Cardiovascular Medicine 1922;2:199
年Havrilesky等分别检测133例I、II期和67例III期的卵巢癌病人和395例健康人群血清中HE4,Glycodelin,MMP7,SLPI, Plau-R, MUC1, Inhibin A,PAI-1和CA125的水平，并以HE4水平为对照，结果表明,HE4在卵巢癌不同期别中的敏感性不同,I/II和III期中的敏感性分别为62.4%-82.7% 和74.6%-92.5%,其特异性为86.3%-96.0%，均优于上述任何一项血清标志物。同年Moore等对233例盆腔包块患者（包括67
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