3-deazaneplanocin A (DZNeP) HCl

製品コード:S7120 別名:NSC 617989 HCl

For research use only.

3-deazaneplanocin A HCl (DZNeP, NSC 617989), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.

3-deazaneplanocin A (DZNeP) HCl化学構造

CAS No. 120964-45-6

サイズ 価格(税別)
JPY 26400
JPY 105500

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(69)

製品安全説明書

Histone Methyltransferase阻害剤の選択性比較

生物活性

製品説明 3-deazaneplanocin A HCl (DZNeP, NSC 617989), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.
特性 Carbocyclic analog of adenosine, and acts as anti-tumor and anti-virus inhibitor of EZH2.
ターゲット
S-adenosylhomocysteine hydrolase [1]
50 pM(Ki)
体外試験

3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle of human acute myeloid leukemia OCI-AML3 cells. 3-Deazaneplanocin A (1.0 μM) induces apoptosis in OCI-AML3 (~50%) and HL-60 cells (~50%), and a more than 90% reduction in colony growth at 48 hr. 3-Deazaneplanocin A depletes EZH2 levels, and inhibits trimethylation of lysine 27 on histone H3 in the HL-60 and OCI-AML3 cells and in primary AML cells. 3-Deazaneplanocin A treatment induces p16, p21, p27, and FBXO32 while depleting cyclin E and HOXA9 levels. 500 nM 3-Deazaneplanocin A induces differentiation of HL-60 to CD11b+ cell by nearly 3-folds time at 48 h. [2] 3-Deazaneplanocin A has excellent activity against several viral types. 3-Deazaneplanocin A is activity against vesicular stomatitis in L929 cells, parainfluenza 3 in H.Ep-2, vaccinia and yellow fever viruses in vero cells with IC50 of 0.2, 3.6, 2.1 and 2.9 μg/mL, respectively. [3] 3-Deazaneplanocin A displays a strongly and uniformly leishmanistatic effect on American Leishmania (L mexicana and L brasiliensis) strains in the study with average ID50 of 96 ng/mL, but shows no inhibition against the several T. cruzi and T. rangeli strains tested with concentrations up to 10 μg/mL. At a dose of 200 ng/mL, 3-Deazaneplanocin A inhibits S-adenosyl-L-3H-methylmethionine and 3-thymidine incorporation by promastigotes after four days. At a dose of 100 ng/mL, 3-Deazaneplanocin A eliminates approximately 56% of the L mexicana and L brasiliensis from infected human macrophages. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human PC3 cells MUTDfZRwfG:6aXRCpIF{e2G7 NXzIRWVIPzJiaB?= MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEmFNUC9PU4{QSEQvF2u NUix[HpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wNVA2QDVpPkK2NFExPTh3PD;hQi=>
human A549 cells MmG1R5l1d3SxeHnjxsBie3OjeR?= NEThO4g4OiCq MnfGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF0yNjRizszNMi=> MkPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyMUC1PFUoRjJ4MEGwOVg2RC:jPh?=
human SNU638 cells M3HpeGN6fG:2b4jpZ:Kh[XO|YYm= M13z[FczKGh? MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUnU3OzhiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFnDOVA:OC57MTFOwG0v NVrvNmF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wNVA2QDVpPkK2NFExPTh3PD;hQi=>
human SKHEP1 cells M3KySmN6fG:2b4jpZ:Kh[XO|YYm= NVzCWXpTPzJiaB?= MlmzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tJTVBzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTBwN{Kg{txONg>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjBzMEW4OUc,OjZyMUC1PFU9N2F-
human MDA-MB-231 cells NV61XWVkS3m2b4TvfIlkyqCjc4PhfS=> NGn0[4M4OiCq MojmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4Phfg+9lCCLQ{WwQVAvOyEQvF2u NUjyPGpDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wNVA2QDVpPkK2NFExPTh3PD;hQi=>
human HCT116 cells MYjDfZRwfG:6aXRCpIF{e2G7 NXrWcmxzPzJiaB?= NH3QN5pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGlEPTB;MD6yOkDPxE1w NFXFeHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkCxNFU5PSd-Mk[wNVA2QDV:L3G+
アッセイ
Methods Test Index PMID
Western blot EZH2 / H3K27me3 ; Suz12 / H3K4me3 / H3K36me2 ; TGFBR1 / TGFBR2 / Smad3 ; EED / p21 / p-RB / p27 / p-CDC2 ; HOXA6 / HOXB3 / HOXC4 / HOXD13 ; p-JNK / JNK / p-p38 / p38 / p-ERK / ERK / p-IκB-α / IκB-α 27223261 23001792 28373289 26579445 26812882 28744016
Immunofluorescence α-tubulin ; F-actin / Paxillin ; EZH2 / Mst1 27226494 23826380 24499724
Growth inhibition assay Cell viability 27223261
体内試験 3-Deazaneplanocin A shows antileukemia activity in vivo. 3-Deazaneplanocin A (1 mg/kg) significantly prolongs survival of mice implanted with AML cells with a median survival of 43 days compared with control group (36 days), which can be further improved by co-treatment with 10 mg/kg pan-HDAC inhibitor (HDI) panobinostat (52 days, median survival). [2] 3-Deazaneplanocin A at the doses of 8 mg/kg shows in vivo antiviral activity against vaccinia virus in a mouse tailpox assay with median of 0.0 poxftail (84% protection). [3] 3-Deazaneplanocin A at the doses ranging from 0.5 to 1.5 mg/kg/day, significantly reduced development of cutaneous leishmanial infection produced in inbred BALB/c mice by L. b. guyanensis inoculation. [4] 3-Deazaneplanocin A induces massively increased interferon-α production in Ebola virus-infected mice. 3-Deazaneplanocin A (s.c. injection of 2 mg/kg postinfection) prevents death in mice infected with 1000 pfu (30 000 LD50) of mouse-adapted EBO-Z. Treatment with 3-Deazaneplanocin A on day 1 reduces mean serum viral titers on day 2 by 100-fold and on day 3 by 100 000-fold, compared with placebo controls, and results in a mean serum IFN-α level of 1420 pg/mL on day 2 and 1830 pg/mL on day 3. [5]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[6]

  • S-adenosylhomocysteine hydrolase activity assay:

    The reaction mixture used for assay of AdoHcyase contains, in a final volume of 0.5 mL, 50 mM potassium phosphate (pH 7.6), 5 mM dithiothreitol, 1 mM EDTA, 10% glycerol, and the enzyme. L-[8- 14C]AdoHcy is used as substrate and 5 units of calf intestinal adenosine deaminase are included. The reaction is stopped by the addition of 100 μL of 5 M formic acid, and the reaction mixture is then poured onto a column (0.8×2.5 cm) of SP-Sephadex C-25, previously equilibrated in 0.1 M formic acid. Each test tube is rinsed with 0.5 mL of 0.1 M formic acid. [14C]Inosine formed is eluted from the column by 3.5 mL of 0.1 M formic acid into a scintillation vial. The radioactivity is determined after the addition of 10 mL of scintillation fluid. The amount of enzyme used is about 105 pU, or 75 ng of the purified enzyme. One unit is the amount of enzyme needed to form 1 pmol of product in 1 min at 37 ℃.

細胞試験:

[2]

  • 細胞株:Human acute myeloid leukemia HL-60
  • 濃度: ~1 μM
  • 反応時間:2 days
  • 実験の流れ:

    Cells are treated with the indicated concentrations of 3-Deazaneplanocin A for 48 hours. After the designated treatments, cells are harvested and washed twice with PBS, and approximately 500 cells are plated in complete Methocult and cultured for 7 to 10 days at 37 ℃ in a 5% CO2 environment. Cells are dyed with crystal violet, and relative colony density is determined by solubilizing the crystal violet dye in 10% acetic acid followed by measurement of absorbance at 450 nm.

動物試験:

[2]

  • 動物モデル:Human acute myeloid leukemia xenografts HL-60
  • 投薬量:1 mg/kg
  • 投与方法:initiated on day 7 and administered twice per week (Tuesday-Thursday) intraperitoneally for 2 weeks

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
Saline
混合させたのち直ちに使用することを推奨します。

30mg/mL

化学情報

分子量 298.73
化学式

C12H14N4O3.HCl

CAS No. 120964-45-6
Storage 3年 -20°C
2年 -80°C in solvent
Smiles C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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