Home Epigenetics Histone Methyltransferase inhibitor 3-deazaneplanocin A (DZNeP) HCl

3-deazaneplanocin A (DZNeP) HCl

Catalog No.S7120 Synonyms: 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 Chemical Structure

CAS No. 120964-45-6

Selleck's 3-deazaneplanocin A (DZNeP) HCl has been cited by 67 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Related Compound Libraries

Biological Activity

Description 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.
Features Carbocyclic analog of adenosine, and acts as anti-tumor and anti-virus inhibitor of EZH2.
Targets
S-adenosylhomocysteine hydrolase [1]
()
50 pM(Ki)
In vitro

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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human PC3 cells NI[2WYJEgXSxdH;4bYPDqGG|c3H5 MmfQO|IhcA>? NVXwephjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTlwM{mg{txONg>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjBzMEW4OUc,OjZyMUC1PFU9N2F-
human A549 cells MVLDfZRwfG:6aXRCpIF{e2G7 NF75N3g4OiCq NFvvc5FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTFwNDFOwG0v NF\4dFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkCxNFU5PSd-Mk[wNVA2QDV:L3G+
human SNU638 cells M3v2VGN6fG:2b4jpZ:Kh[XO|YYm= MonCO|IhcA>? NGHOd2NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUVlV4M{igZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGlEPTB;MD65NUDPxE1w MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjBzMEW4OUc,OjZyMUC1PFU9N2F-
human SKHEP1 cells MX\DfZRwfG:6aXRCpIF{e2G7 MlTLO|IhcA>? NH3OXWhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0iHUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGlEPTB;MD63NkDPxE1w NIDvfWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkCxNFU5PSd-Mk[wNVA2QDV:L3G+
human MDA-MB-231 cells MlrPR5l1d3SxeHnjxsBie3OjeR?= M{focVczKGh? MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H589yNKEmFNUC9NE4{KM7:TT6= M3jud|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEGwOVg2Lz5{NkCxNFU5PTxxYU6=
human HCT116 cells M1jjbmN6fG:2b4jpZ:Kh[XO|YYm= MknVO|IhcA>? MlHSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTBwMk[g{txONg>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjBzMEW4OUc,OjZyMUC1PFU9N2F-
Click to View More Cell Line Experimental Data
Assay
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
In vivo 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]

Protocol (from reference)

Kinase Assay:

[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 ℃.
Cell Research:

[2]
  • Cell lines: Human acute myeloid leukemia HL-60
  • Concentrations: ~1 μM
  • Incubation Time: 2 days
  • Method:

    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.
Animal Research:

[2]
  • Animal Models: Human acute myeloid leukemia xenografts HL-60
  • Dosages: 1 mg/kg
  • Administration: initiated on day 7 and administered twice per week (Tuesday-Thursday) intraperitoneally for 2 weeks

Solubility (25°C)

In vitro

 DMSO 52 mg/mL
(174.07 mM)
Water 52 mg/mL
(174.07 mM)
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

 30mg/mL

Chemical Information

Molecular Weight 298.73
Formula

C12H14N4O3.HCl
CAS No. 120964-45-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy 3-deazaneplanocin A (DZNeP) HCl | 3-deazaneplanocin A (DZNeP) HCl supplier | purchase 3-deazaneplanocin A (DZNeP) HCl | 3-deazaneplanocin A (DZNeP) HCl cost | 3-deazaneplanocin A (DZNeP) HCl manufacturer | order 3-deazaneplanocin A (DZNeP) HCl | 3-deazaneplanocin A (DZNeP) HCl distributor