3-Deazaneplanocin,DZNep

3-Deazaneplanocin,DZNep

Catalog Number:
L002368349APE
Mfr. No.:
APE-A1905
Price:
$228
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      • Overview
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          Background

          3-Deazaneplanocin is a highly potent inhibitor of S-adenosylhomocysteine hydrolase with Ki value of 0.05 nM [1].
          3-Deazaneplanocin was synthesized as an inhibitor of S-adenosylhomocysteine hydrolase. It is an analog of adenosine and inhibits S-adenosylhomocysteine hydrolase through competing with the substrate, adenosine. 3-Deazaneplanocin was not so that potent in cell growth inhibition. 10 μM 3-Deazaneplanocin treatment resulted in moderate cell growth reduction in HL-60 cells. In HCC cell lines Huh1 and Huh7, 3-Deazaneplanocin inhibited growth and non-adherent sphere formation dose-dependently. It decreased the epithelial cell adhesion molecule EpCAMhigh fraction from 49.0% to 12.5% in Huh1 cells and from 44.4% to 11.6% in Huh7 cells. Moreover, in mice implanted with Huh7 cells, administration of 3-Deazaneplanocin suppressed tumor initiation and growth via directly affecting the growth and self-renewal of tumor-initiating cells [1, 2].

          [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.

      • Properties
        • Alternative Name
          DZNep, 3-Deazaneplanocin A,NSC 617989,NSC617989; (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol
          CAS Number
          102052-95-9
          Molecular Formula
          C12H24N4O3
          Molecular Weight
          262.26
          Appearance
          A crystalline solid
          Purity
          98.00%
          Solubility
          insoluble in EtOH; ≥17.07 mg/mL in DMSO; ≥17.43 mg/mL in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 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

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