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CAS No.: 120964-45-6

3-Deazaneplanocin A HCl/3-去氮腺嘌呤A盐酸盐 Catalog No. CSN13890

Synonyms: DZNep hydrochloride;NSC 617989 hydrochloride;3-Deazaneplanocin hydrochloride

3-Deazaneplanocin A HCl is a cyclopentanyl analog of 3-deazaadenosine that potently interferes with SAH, a component of the methionine cycle, which causes cellular SAH levels to increase, thus repressing the activity of S-adenosyl-l-methionine–dependent histone lysine methyltransferase activity.

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技术信息

生物活性

靶点 Adenosylhomocysteinase

Ki:50pM
描述3-Deazaneplanocin A is a cyclopentanyl analog of 3-deazaadenosine that potently interferes with SAH, a component of the methionine cycle, which causes cellular SAH levels to increase, thus repressing the activity of S-adenosyl-l-methionine–dependent histone lysine methyltransferase activity^[1]. Thus, the effect of 3-Deazaneplanocin A in inhibiting histone methylation is not specific to EZH2. Treatment with 5 μM of 3-Deazaneplanocin A for 72h led to a global decrease in most histone examined, including H3K27me3, H3K9me2, H3K79me3, H4K20me3, H3K4me3, H3K9me1, H3R2me2 and H3K27me1, with most reduction on H3K27me3 and H4K20me3, in MCF-7 cells, as well as slight decrease of EZH2^[1]. Treatment with 5 µM 3-Deazaneplanocin A for 48 and 72h depletes EZH2 proteins as well as inhibits histone H3-K27 methylation, and induces apoptotic cell death in MCF-7 and HCT116 cells. 3-Deazaneplanocin A treatment removes the binding of PRC2 to their target genes and increases the binding of RNA Pol II, thus increases recruitment of RNA Pol II and transcriptional activation of these PRC2 target genes, such as FBXO32, LAMB3, PLAU, and PPP1R15A, in MCF-7 cells, MDA-MB-468, SK-BR-3 and T47D cell lines sensitive to DZNep-induced cell death^[2]. Recently, it was found that 3-Deazaneplanocin A can enhance Oct4 expression in chemically induced pluripotent stem cells^[3].
作用机制Deazaneplanocin A is a cyclopentanyl analog of 3-deazaadenosine, thus functioning as a SAH hydrolase inhibitor of methyltransferases^[1].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A549 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=1.4 μM.	26010585
human HCT116 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=0.26 μM.	26010585
human MDA-MB-231 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay， IC50=0.3 μM.	26010585

动物研究

剂量

Mice^[4]: 1 mg/kg (i.p.); min = 3.75 mg/kg , max = 25 mg/kg (s.c.)

给药途径

i.p., s.c.

动物药代数据

Animal	Rats^[5]
Dose	5 mg/kg
Administration	i.v.
T_1/2	1 h
Vss	0.63 L
CL	0.59 L/h
AUC_0→12h	2.7 h·μg/ml

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3475 mL
- 16.7375 mL
- 33.4750 mL
- 5 mM
- 0.6695 mL
- 3.3475 mL
- 6.6950 mL
- 10 mM
- 0.3348 mL
- 1.6738 mL
- 3.3475 mL

技术信息

CAS号

120964-45-6

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H15ClN4O3

运输

蓝冰

分子量

298.73

别名

DZNep hydrochloride;NSC 617989 hydrochloride;3-Deazaneplanocin hydrochloride;DZNep HCl;NSC 617989 HCl;3-Deazaneplanocin A (hydrochloride);2,3-DMMC;3-deazaneplanocin A HCl;3-deazaneplanocin A hydrochloride;DZNep;NSC 617989;3-去氮腺嘌呤A盐酸盐

溶解度

DMSO	56.0 mg/mL (187.5 mM)
Water	55.0 mg/mL (184.1 mM)

动物实验配方

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3-Deazaneplanocin A HCl/3-去氮腺嘌呤A盐酸盐 Catalog No. CSN13890

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