3-Deazaneplanocin A (DZNep) hydrochloride (Synonyms: 2,3DMMC) |
| カタログ番号GC17907 |
3-デアザネプラノシンA(DZNep)塩酸塩（3-Deazaneplanocin A (DZNep) hydrochloride）はアデノシンアナログであり、無細胞試験において競合的S-adenosylhomocysteine hydrolaseの阻害剤である（Ki値は50 pM）。
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-デアザネプラノシンA(DZNep)塩酸塩（3-Deazaneplanocin A (DZNep) hydrochloride）はアデノシンアナログであり、無細胞試験において競合的S-adenosylhomocysteine hydrolaseの阻害剤である（Ki値は50 pM）。細胞内にAdoHcyが蓄積し、S-adenosyl-l-methionine依存性KMTase活性の阻害につながる。3-デアザネプラノシンA(DZNep)塩酸塩はメチルトランスフェラーゼの活性を抑制し、mRNAsの低メチル化を生じた。
3-デアザネプラノシンA(DZNep)塩酸塩(100-750 nmol/L; 48 hours)処理は細胞周期停止とアポトーシスを誘導し、AML細胞のクロロゲン生存率を低減した。3-デアザネプラノシンA(DZNep)塩酸塩は乳がん細胞においてPRC2複合体の発見レベルを低下させ、それに伴い、3Me H3K27マークが消失し、エピジェネティックにサイレンシングされた標的の抑制が解除された。3-デアザネプラノシンA(DZNep)塩酸塩(10-6M-10-5M ;2 days)は細胞培養において水疱性口内炎、パラインフルエンザ3型、黄熱、ワクシニアウイルスに対して優れた抗ウィルス活性を示した。
3-デアザネプラノシンA(DZNep)塩酸塩(1 mg/kg; i.p.; 2 weeks)とpanobinostatはAML細胞のアポトーシスを誘導し、HL-60白血病非肥満性糖尿病／重症免疫不全マウスの生存率を増加した。3-デアザネプラノシンA(DZNep)塩酸塩(i.p.; 0.5-1.5 mg/kg/d; 2 weeks)はL.b.ガイアネンシス接種による近交系BALB/cマウスの皮膚におけるリーシュマニア感染の発症率を減少した。
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.
| 細胞実験[1]: | |
細胞株 | OCI-AML3 細胞 |
準備方法 | 細胞は一定濃度のDZNepを24時間処理した。 |
反応条件 | DZNep (0/1.0 µM); 24 h |
アプリケーション | OCI-AML3 細胞をDZNep (1.0 µM)で処理すると、細胞G0/G1期の蓄積が有意に増加し、それと同時にS期とG2/M期の細胞数が減少した。 |
| 動物実験 [2]: | |
動物モデル | メス非肥満性糖尿病／重症免疫不全(NOD/SCID)マウス |
準備方法 | HL-60細胞(5 million)をマウス尾静脈に注射した。次の投与はマウス7匹1コホートで治療を行う：ビークル単独、1 mg/kg DZNep、10 mg/kg PS、DZNepとPS。治療は7日目に開始する。DZNepは週2回、2週間腹腔内投与し、その後投与を中止した。 |
投与形態 | 1 mg/kg DZNep; i.p.;週2回で2週間 |
アプリケーション | DZNepを投与したNOD/SCIDマウスはHL-60細胞に起因するAMLからの生存率が有意に改善した。 |
References:
[1]. 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.
[2].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.
| Cas No. | 120964-45-6 | SDF | |
| 同義語 | 2,3DMMC | ||
| Chemical Name | (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol;hydrochloride | ||
| Canonical SMILES | C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl | ||
| Formula | C12H14N4O3.HCl | M.Wt | 298.73 |
| 溶解度 | ≥ 14.9mg/mL in DMSO, ≥ 18.32 mg/mL in Water with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3475 mL | 16.7375 mL | 33.475 mL |
| 5 mM | 0.6695 mL | 3.3475 mL | 6.695 mL |
| 10 mM | 0.3348 mL | 1.6738 mL | 3.3475 mL |
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Quality Control & SDS
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- Purity: >99.50%
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