3-Deazaneplanocin,DZNep
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
3- Deazaneplanocin是一种高效的S-腺苷高半胱氨酸水解酶抑制剂，Ki值为0.05 nM[1]。
3- Deazaneplanocin是腺苷的类似物，与底物腺苷竞争抑制S-腺苷高半胱氨酸水解酶。3-Deazaneplanocin对细胞生长的抑制作用较弱。在HL-60细胞中，10 μM的3-Deazaneplanocin处理只能适度减少细胞的生长。在HCC肝癌细胞系Huh1和Huh7中，3-Deazaneplanocin剂量依赖性地抑制细胞的生长和非粘附球的形成。在Huh1细胞中，3-Deazaneplanocin将上皮细胞粘附分子EpCAM从49.0％减少到12.5%。在Huh7细胞中，3-Deazaneplanocin将EpCAM从44.4%减少到11.6%。在异种移植Huh7细胞的小鼠中，3-Deazaneplanocin通过直接影响肿瘤起始细胞的生长和自我更新，从而抑制肿瘤的发生和生长[1, 2]。
参考文献：
[1] Glazer R I, Hartman K D, Knode M C, et al. 3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochemical and biophysical research communications, 1986, 135(2): 688-694.
[2] Chiba T, Suzuki E, Negishi M, et al. 3-Deazaneplanocin A is a promising therapeutic agent for the eradication of tumor-initiating hepatocellular carcinoma cells. International Journal of Cancer, 2012, 130(11): 2557-2567.
- 1. Weiyun Wang, Shaofang Ren, et al. "Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production." EMBO J. 2021 Jun 1;40(11):e106771. PMID:33909912
- 2. Xu W, Huang M, et al. "The Role of CHK1 Varies with the Status of Oestrogen-receptor and Progesterone-receptor in the Targeted Therapy for Breast Cancer." Int J Biol Sci. 2020;16(8):1388-1402. PMID:32210727
- 3. Bassem Merit,Shoucri. "Retinoid X Receptor Activation by the Endocrine Disruptor Tributyltin Promotes Adipose Lineage Commitment and Perturbs Adipocyte Function" UNIVERSITY OF CALIFORNIA.2018.
- 4. Hardik Rameshchandra Mody. "Investigation of Micro-RNA-based Approaches to Overcome Epithelial-Mesenchymal Transition in Pancreatic Cancer" Ohio State University.2017. PMID:29498802
- 5. Lin B, Coleman JH, et al."Injury Induces Endogenous Reprogramming and Dedifferentiation of Neuronal Progenitors to Multipotency." Cell Stem Cell. 2017 Nov 20. pii: S1934-5909(17)30375-2. PMID:29174332
- 6. Shi X, Tasdogan A, et al. "The abundance of metabolites related to protein methylation correlates with the metastatic capacity of human melanoma xenografts." Sci Adv. 2017 Nov 1;3(11):eaao5268. PMID:29109980
- 7. Bassem M. Shoucri, Eric S. Martinez, et al. "Retinoid X receptor activation alters the chromatin landscape to commit mesenchymal stem cells to the adipose lineage." Endocrinology. 2017 Jul.
- 8. Yang SZ, Xu F, et al. "The long non-coding RNA HOTAIR enhances pancreatic cancer resistance to TNF-related apoptosis-inducing ligand." J Biol Chem. 2017 Jun 23;292(25):10390-10397. PMID:28476883
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 262.26 |
| Cas No. | 102052-95-9 |
| Formula | C12H24N4O3 |
| Synonyms | DZNep, 3-Deazaneplanocin A,NSC 617989,NSC617989 |
| Solubility | insoluble in EtOH; ≥17.07 mg/mL in DMSO; ≥17.43 mg/mL in H2O |
| Chemical Name | (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol |
| SDF | Download SDF |
| Canonical SMILES | C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
人急性骨髓性白血病（AML）细胞 |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
100-750 nM；24-72 h |
|
应用 |
在培养的和原代AML细胞中，DZNep诱导细胞凋亡。在AML HL-60和OCI-AML3细胞中，DZNep耗尽EZH2水平，抑制组蛋白H3赖氨酸27（H3K27）的三甲基化。在cyclin E和HOXA9水平耗尽之后，DZNep诱导p16、p21、p27和FBXO32的水平。 |
| 动物实验[2]： | |
|
动物模型 |
Sprague-Dawley大鼠（120-140 g） |
|
剂量 |
5 μM；实验前24小时处理，随饮食口服。 |
|
应用 |
在非酒精性脂肪性肝病（NAFLD）小鼠模型中，DZNep显著减少EZH2的表达和活性，增加脂质沉积、炎症分子和microRNAs。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: 1. Fiskus W1, Wang Y, Sreekumar A et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 2009 Sep 24;114(13):2733-43. 2. Vella S, Gnani D, Crudele A et al. EZH2 down-regulation exacerbates lipid accumulation and inflammation in vitro and in vivo NAFLD.Int J Mol Sci. 2013 Dec 12;14(12):24154-68. |
|
| 描述 | 3-deazaneplanocin A (DZNeP)，腺苷类似物，是S-腺苷高半胱氨酸水解酶（S-adenosylhomocysteine hydrolase）的竞争性抑制剂，Ki值为50 pM。 | |||||
| 靶点 | S-adenosylhomocysteine hydrolase | |||||
| IC50 | 50 pM (Ki) | |||||
化学结构
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
