生物活性

DZNep is a potent ENZ2 inhibitor. When tested with human acute myeloid leukemia (AML) HL-60 and OCI-AML3 cell lines, administration of DZNep induced cell apoptosis by depleting ENZ2, cyclin E and HOXA9 expressions and inducing p16, p21,p27 and FBXO32 expressions in a dose-dependent manner.

体外研究

体内研究

激酶实验

细胞实验

~1 μM

动物实验

1 mg/kg 实验第7天开始，每周腹腔处理两次（周二-周四），持续2周

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Glazer RI, et al. Biochem Pharmacol, 1986, 35(24), 4523-4527.
[2] Tan et al (2007) Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev. 21 1050.
[3] Miranda et al (2009) DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation. Mol.Cancer Ther. 8 1579.
[4] Hou et al (2013) Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science 341 651.
[5] Tseng et al (1989) Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities. J.Med.Chem. 32 1442.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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