3-deazaneplanocin A (DZNeP) HCl

Catalog No.S7120 Synonyms: NSC 617989 HCl

3-deazaneplanocin A (DZNeP) HCl Chemical Structure

Molecular Weight(MW): 298.73

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

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Cited by 11 Publications

6 Customer Reviews

  • H3K27me3 inhibitors inducing cell differentiation in the MDS-derived erythroid/myeloid cell line and primary MDS bone marrow cells via reducing H3K27me3 and increasing the expressions of PU.1 and its downstream genes. (a) ChIP experiments show a marked decrease in H3K27me3 at the PU.1 enhancer in the OCI-M2 cells treated with DZNep, compared with that in the cells treated with dimethyl sulfoxide (DMSO). (b) RT-PCRs show a significant increase in the expression of PU.1 mRNA in the OCI-M2 cells treated with DZNep in a dose-dependent manner. (c) Flow cytometric studies show that an increase in the expression of glycophorin A/B, a marker associated with erythroid differentiation, in the OCI-M2 cells treated with 0.25 μM of DZNep for 6 days. Red, isotype control; blue, no drug treatment (DMSO only); green, plus drug. (d) Increased PU.1 mRNA expression in primary MDS bone marrow cells treated with DZNep, compared with that in DMSO control. (e) Increased CD18 mRNA expression in primary MDS bone marrow cells treated with DZNep, compared with that in DMSO control. The primary bone marrow cells were from three cytogenetically normal MDS patients, which had marked trilineage dysplasia with varying numbers of blasts (case-1 with 10% blasts, case-2 with 4.6% blasts and case-3 with 11% blasts). The MDS bone marrow cells were treated with 1 μM DZNep or DMSO (control) for 24 h. The levels of PU.1 and CD18 mRNAs were measured by Q-RT-PCRs, while TBP mRNA was used for the internal normalization

    Leukemia, 2013, 1291-1300. 3-deazaneplanocin A (DZNeP) HCl purchased from Selleck.

    Photomicrographs illustrate immunofluorescent staining of NGAL in kidney tissues collected at 48 h after sham and IR injury with or without 3-DZNep administration in C57/black mice.

    Cell Death Dis, 2018, 9(11):1067. 3-deazaneplanocin A (DZNeP) HCl purchased from Selleck.

  • EZH2 knockdown in pancreatic cancer cells inhibits cell migration and invasion. A, B. The migration and invasion ability of pancreatic cancer cell lines AsPC-1(A), CFPAC-1(B) with EZH2 knockdown. The scales represent 50μm. C, D. we examined the E-cadherin, ZEB1 and Snail expressions after using EZH2 RNAi, DZNeP and EPZ-6438. “*”represent P<0.05 when compared with control group.

    Oncotarget, 2016, 7(10):11194-207. 3-deazaneplanocin A (DZNeP) HCl purchased from Selleck.

    HSC‐T6 cells were treated with TGF‐β1 or TGF‐β1 plus DZNep. Real‐time PCR was performed to assess the mRNA expression level of α‐SMA at the three groups. HSC‐T6 cells were treated with TGF‐β1 or TGF‐β1 plus DZNep. Western blotting was carried out to assess the protein levels of EZH2 and α‐SMA at the three groups.

    J Cell Mol Med, 2017, 21(10):2317-2328. 3-deazaneplanocin A (DZNeP) HCl purchased from Selleck.

  • (A) Representative Western blot images for the analysis of histone H3 repressive methylation marks in Cr(VI)-transformed cells. Cells were treated with vehicle control, a G9a inhibitor BIX01294 (2.5 μM) or an EZH2 inhibitor DZNeP (0.25 μM) for 72 h, and harvested for Western blot analysis. (B) Quantitation of effects of inhibition of G9a or EZH2 on soft agar colony and suspension culture sphere formation by Cr(VI)-transformed cells. Cells were treated with vehicle control, a G9a inhibitor BIX01294 (2.5 μM) or an EZH2 inhibitor DZNeP (0.25 μM) for 72 h, and harvested for soft agar colony and suspension culture sphere formation assay. Results are expressed as relative colony or sphere formation compared to vehicle-treated BEAS-2B-Cr(VI) cells (100%). Data are presented as mean ± SD (n=3). *p< 0.05, compared to vehicle-treated group. Similar results were obtained in two additional experiments.

    Toxicol Appl Pharmacol, 2018, 342:22-30. 3-deazaneplanocin A (DZNeP) HCl purchased from Selleck.

    Tumor samples from three distinct groups underwent immunohistochemistry for STAT3, p-STAT3 (Tyr705), EZH2, H3K27me3, MMP2, MMP6, E-cadherin, N-cadherin and Vimentin expression (scale bar, 100 μm; magnification, ×200).

    Int J Oncol, 2018, 52(4):1149-1164. 3-deazaneplanocin A (DZNeP) HCl purchased from Selleck.

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description 3-deazaneplanocin A (DZNeP)HCl, 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 HCT116 cells M2r5eWN6fG:2b4jpZ:Kh[XO|YYm= NVHtV3BnPzJiaB?= NULGbVJWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBKSzVyPUCuNlYh|ryPLh?= NEfFemwzPjBzMEW4OS=>
human MDA-MB-231 cells NEjZXJNEgXSxdH;4bYPDqGG|c3H5 MkPDO|IhcA>? M4TBdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZnwxIxiSVO1NF0xNjNizszNMi=> NVu4[IxFOjZyMUC1PFU>
human SKHEP1 cells MV\DfZRwfG:6aXRCpIF{e2G7 NIrGN2E4OiCq NFTzTnNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0iHUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGlEPTB;MD63NkDPxE1w MoLWNlYxOTB3OEW=
human SNU638 cells NU[yTnZDS3m2b4TvfIlkyqCjc4PhfS=> M{fZ[FczKGh? M4fJXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPXTZ|ODDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OD1yLkmxJO69VS5? MmfpNlYxOTB3OEW=
human A549 cells NUHBZ|Y5S3m2b4TvfIlkyqCjc4PhfS=> Mkj0O|IhcA>? NID0TFlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTFwNDFOwG0v NWnV[5ZiOjZyMUC1PFU>
human PC3 cells NHfMS5JEgXSxdH;4bYPDqGG|c3H5 MXS3NkBp M4C2ZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF06NjN7IN88UU4> Mlm3NlYxOTB3OEW=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
EZH2 / H3K27me3; 

PubMed: 27223261     


DZNep decreased the expression of EZH2 and H3K27me3 in osteosarcoma cells in a dose-dependent manner.

Suz12 / H3K4me3 / H3K36me2; 

PubMed: 23001792     


A marked decrease in H3K27me3 levels in DZNep treated HT29 and SW480 cells compared to untreated controls. While the effect of DZNep was relatively specific for H3K27me3 inhibition in HT29 cells, DZNep also reduced H3K4me3 and H3K36me2 marks in SW480 cells. As reported by others, DZNep treatment caused a decrease in Suz12 protein levels in SW480 cells, whereas Suz12 protein level was unaffected in HT29 cells

TGFBR1 / TGFBR2 / Smad3; 

PubMed: 28373289     


DZNep decreased TGFBR1 and TGFBR2 but not Smad3 protein levels in a dose-dependent fashion in pancreatic cancer. 

EED / p21 / p-RB / p27 / p-CDC2; 

PubMed: 26579445     


Relative protein expression levels affected by DZNep in HCT116 cells. The cells were treated with 5 μmol/L DZNep for 72 h before being subjected to immunoblot assay.

HOXA6 / HOXB3 / HOXC4 / HOXD13; 

PubMed: 26812882     


Western blot analysis showed that both DZNep and EPZ005687 reduced EZH2 expression and H3K27me3 levels. 

p-JNK / JNK / p-p38 / p38 / p-ERK / ERK / p-IκB-α / IκB-α; 

PubMed: 28744016     


DZNep reduced MAPK pathway activation by IL-1β. Primary chondrocytes were treated or not with DZNep (1 µM) in the presence of IL-1β (1ng/mL) for 0min, 5min or 10min. Afer treatment, proteins were extracted, and levels of P-JNK and JNK, P-p38 and p38, P-ERK and ERK, P-IκB-α and IκB-α were determined in cells by western blotting.

27223261 23001792 28373289 26579445 26812882 28744016
Immunofluorescence
α-tubulin; 

PubMed: 27226494     


Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.

F-actin / Paxillin; 

PubMed: 23826380     


DZNep treatment impaired actin cytoskeleton and caused cell shrinkage in MHCC97L cells. Stress fiber was stained with FITC-conjugated phalloidin and focal adhesions were stained with anti-paxillin antibody. Nuclei were counterstained with DAPI. Mock-treated cells showed organized bundles of stress fibers and well attached paxillin. DZNep-treated cells shrank and lost proper actin cytoskeleton network.

EZH2 / Mst1; 

PubMed: 24499724     


Co-IF staining of EZH2 and MST1 protein in C4–2 cells treated with DMSO or 5 µM DZNep for 72h in serum-fed growth conditions. Alexa Fluor 488 stained MST1 (green), Alexa Fluor 568 stained EZH2 (red), and DAPI stained cell nuclei (blue). Magnification is 20x. Micrographs are representative of multiple images from two independent experiments.

27226494 23826380 24499724
Growth inhibition assay
Cell viability; 

PubMed: 27223261     


DZNep inhibited osteosarcoma cell proliferation. Cells were treated with DZNep at the indicated concentrations. The relative sensitivity of each line to DZNep was determined by the MTT assay.

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

Kinase Assay:

[6]

+ Expand

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]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[2]

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

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.73
Formula

C12H14N4O3.HCl

CAS No. 120964-45-6
Storage powder
in solvent
Synonyms NSC 617989 HCl

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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.

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID