3-Deazaneplanocin A (DZNep) hydrochloride (Synonyms: 2,3DMMC) |
| カタログ番号GC17907 |
リジンメチルトランスフェラーゼEZH2の阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120964-45-6
Sample solution is provided at 25 µL, 10mM.
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3-Deazaneplanocin A (DZNep) hydrochloride is an adenosine analogue and is a competitive S-adenosylhomocysteine hydrolase inhibitor with a Ki of 50 pM in cell-free tests.This results in the intracellular accumulation of AdoHcy, which leads to inhibition of the S-adenosyl-l-methionine dependent KMTase activity[1-2,5].3-Deazaneplanocin A (DZNep) hydrochloride has also been shown to inhibit the activity of the methyltransferases, resulting in undermethylation of mRNAs[3].
3-Deazaneplanocin A (DZNep) hydrochloride (100-750 nmol/L; 48 hours) treatment induces cell-cycle arrest and apoptosis, and markedly reduces clonogenic survival of AML cells[4]. 3-Deazaneplanocin A (DZNep) hydrochloride was reported to deplete the expression levels of the PRC2 complex in breast cancer cells with concomitant loss of 3Me H3K27 mark and derepression of epigenetically silenced targets[6]. 3-Deazaneplanocin A (DZNep) hydrochloride(10-6M-10-5M ;2 days)displayed excellent antiviral activity in cell culture against vesicular stomatitis, parainfluenza type 3, yellow fever, and vaccinia viruses[1].
3-Deazaneplanocin A (DZNep) hydrochloride (1 mg/kg; i.p.; 2 weeks) and panobinostat induced apoptosis of AML cells and significantly improved the survival rate of non-obese diabetic/severely immunodeficient mice with HL-60 leukemia [4]. 3-Deazaneplanocin A (DZNep)(i.p.; 0.5-1.5 mg/kg/d; 2 weeks)can significantly reduce the incidence of leishmania infection in skin of inbred BALB/c mice induced by L. b. guyanensis inoculation [7].
References:
[1]. Glazer RI, Hartman KD, et,al.3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochem Biophys Res Commun. 1986 Mar 13;135(2):688-94. doi: 10.1016/0006-291x(86)90048-3. PMID: 3457563.
[2]. Bray M, Driscoll J, et,al.Treatment of lethal Ebola virus infection in mice with a single dose of an S-adenosyl-L-homocysteine hydrolase inhibitor. Antiviral Res. 2000 Feb;45(2):135-47. doi: 10.1016/s0166-3542(00)00066-8. PMID: 10809022.
[3]. Jiang X, Tan J, et,al. DACT3 is an epigenetic regulator of Wnt/beta-catenin signaling in colorectal cancer and is a therapeutic target of histone modifications. Cancer Cell. 2008 Jun;13(6):529-41. doi: 10.1016/j.ccr.2008.04.019. PMID: 18538736; PMCID: PMC2577847.
[4]. Fiskus W, Wang Y, 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. doi: 10.1182/blood-2009-03-213496. Epub 2009 Jul 28. PMID: 19638619; PMCID: PMC2756128.
[5]. Tseng CK, Marquez VE, Fuller RW, Goldstein BM, Haines DR, McPherson H, Parsons JL, Shannon WM, Arnett G, Hollingshead M, et al. 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. 1989 Jul;32(7):1442-6. doi: 10.1021/jm00127a007. PMID: 2544721.
[6]. Tan J, Yang X, et,al. Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev. 2007 May 1;21(9):1050-63. doi: 10.1101/gad.1524107. Epub 2007 Apr 16. PMID: 17437993; PMCID: PMC1855231.
[7]. Avila JL, Avila A, et,al.Specific inhibitory effect of 3-deazaneplanocin A against several Leishmania mexicana and L. braziliensis strains. Am J Trop Med Hyg. 1997 Oct;57(4):407-12. doi: 10.4269/ajtmh.1997.57.407. PMID: 9347954.
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