3-Deazaneplanocin A hydrochloride
Based on 35 publication(s) in Google Scholar
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 120964-45-6
- Formula: C12H15ClN4O3
- Molecular Weight:298.73
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) 3-Deazaneplanocin A hydrochloride
More- Cell Stem Cell. 2025 Oct 2;32(10):1545-1562.e12. [Abstract]
- Cell Stem Cell. 2025 Oct 2;32(10):1509-1527.e9. [Abstract]
- Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
- Nat Commun. 2021 Feb 23;12(1):1237. [Abstract]
- J Clin Invest. 2025 Jul 22;135(19):e190215. [Abstract]
- Cell Death Dis. 2025 Apr 14;16(1):291. [Abstract]
- Cell Death Dis. 2020 Oct 23;11(10):906. [Abstract]
- J Immunother Cancer. 2019 Nov 14;7(1):300. [Abstract]
- J Exp Med. 2026 Jan 5;223(1):e20250603. [Abstract]
- Cell Death Discov. 2024 Jul 28;10(1):341. [Abstract]
- J Am Soc Nephrol. 2016 Jul;27(7):2021-34. [Abstract]
- Apoptosis. 2020 Oct;25(9-10):697-714. [Abstract]
- Cell Rep. 2023 May 23;42(6):112550. [Abstract]
- Int Immunopharmacol. 2022 May:106:108612. [Abstract]
- J Mol Cell Cardiol. 2019 Oct:135:119-133. [Abstract]
- Cancers (Basel). 2022 Jul 23;14(15):3600. [Abstract]
- Cell Signal. 2024 Mar:115:111029. [Abstract]
- FASEB J. 2025 May 15;39(9):e70605. [Abstract]
- J Pharmacol Exp Ther. 2019 Sep;370(3):490-503. [Abstract]
- Lab Invest. 2021 May;101(5):600-611. [Abstract]
- Exp Mol Pathol. 2020 Feb:112:104344. [Abstract]
- AMB Express. 2025 Jul 26;15(1):110. [Abstract]
- Exp Eye Res. 2025 Sep 26:110670. [Abstract]
- Genes (Basel). 2024 Sep 13;15(9):1206. [Abstract]
- Cell Reprogram. 2017 Dec;19(6):363-371. [Abstract]
- Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067. [Abstract]
- Cells Tissues Organs. 2020;209(4-6):227-235. [Abstract]
- bioRxiv. 2025 Sep 14.
- bioRxiv. 2024 July 27.
- bioRxiv. 2024 May 18.
- bioRxiv. 2023 Apr 21:2023.04.19.537556. [Abstract]
- Research Square Print. September 13th, 2022.
- Università degli Studi di CAGLIARI. 2021 May.
- Research Square Preprint. 2020 May.
- Patent. US20180263995A1.
Customer Validation & Images
-
WB
-
WB
-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
All Histone Methyltransferase Isoforms
More
Biological Activity
|
EZH2 |
3-Deazaneplanocin A (DZNep) hydrochloride is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 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 (P<0.05). Treatment with 3-Deazaneplanocin A (200 nM to 2.0 μM) for 48 hours, dose dependently, inhibits colony growth of OCI-AML3 and HL-60 cells[1].
3-Deazaneplanocin A (DZNep) hydrochloride reduces the expression of EZH2, especially after 72 hours (e.g. 48%, 32% and 36% reduction of EZH2 in PANC-1, MIA-PaCa-2 and LPc006 cells, respectively)[2].
3-Deazaneplanocin A (DZNep) hydrochloride shows minimal growth inhibition in PANC-1 cells. More than 50% of these cells are still growing after exposure at the highest concentration (20 μM). MIA-PaCa-2 and LPc006 cells are much more sensitive, with IC0 values of 1.0±0.3 and 0.10±0.03 μM, respectively[2]. 3-Deazaneplanocin A (DZNep) hydrochloride causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC0 values range from 0.08 to 0.24 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 120964-45-6
-
Appearance Solid
-
Molecular Weight 298.73
-
Formula C12H15ClN4O3
-
Color White to light brown
-
SMILES
O[C@@H]1[C@H](O)C(CO)=C[C@H]1N2C=NC3=C2C=CN=C3N.[H]Cl
-
Synonyms
DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (35)
-
Journal Impact Factor
-
Most Recent
-
Cell Stem Cell
Transgene-free generation of mouse post-gastrulation whole embryo models solely from naive ESCs and iPSCs. [Abstract]2025 Oct 2;32(10):1545-1562.e12. PMID: 40780191 -
Cell Stem Cell
An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193 -
Nat Commun
EZH2 depletion potentiates MYC degradation inhibiting neuroblastoma and small cell carcinoma tumor formation. [Abstract]2022 Jan 10;13(1):12. PMID: 35013218
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
Immunoblot of MYCN in the presence of various EZH2 inhibitors. Kelly cells were respectively treated with 5 μM of 3-Deazaneplanocin A hydrochloride, GSK126 or EPZ6438 for 48 h before subjected to immunoblotting.
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
Proliferation of Kelly cells was measured upon administration of 5 μM of 3-Deazaneplanocin A hydrochloride (5 days), GSK126 or EPZ6438.
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
Proliferation of Kelly cells was measured upon 3-Deazaneplanocin A hydrochloride treatment (5 μM, 5 days) with or without ectopic expression of the MYCN T50A.
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
Kelly xenografts were subjected to 3-Deazaneplanocin A hydrochloride (0.75-6 mg/kg) or GSK126 treatments at the indicated doses. Images of subcutaneous tumors (n = 3 per group) under various treatments are shown.
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
Kaplan-Meier survival plot of tumor-bearing TH-MYCN+/+ mice treated with 3-Deazaneplanocin A hydrochloride (3 mg/kg) or GSK126 (50 mg/kg). Significant difference between the 3-Deazaneplanocin A hydrochloride-treated group versus control was determined by log-rank test.
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12. [Abstract]
Immunohistochemistry detection of Ezh2, MYCN, and H3K27me3 upon 3-Deazaneplanocin A hydrochloride (3 mg/kg) or GSK126 treatment.
-
Nat Commun
Acquired cancer cell resistance to T cell bispecific antibodies and CAR T targeting HER2 through JAK2 down-modulation. [Abstract]2021 Feb 23;12(1):1237. PMID: 33623012
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 23;12(1):1237. [Abstract]
BT-R cells were treated with the specified compound 3-Deazaneplanocin A (DZNEP: 5 μM) for 48 hours. Then, the expression level of JAK2 mRNA was determined by RT-PCR and normalized to the expression level in the vector-treated cells.
-
J Clin Invest
Coenzyme A protects against ferroptosis via CoAlation of mitochondrial thioredoxin reductase. [Abstract]2025 Jul 22;135(19):e190215. PMID: 40694424 -
Cell Death Dis
A targetable antioxidant defense mechanism to EZH2 inhibitors enhances tumor cell vulnerability to ferroptosis. [Abstract]2025 Apr 14;16(1):291. PMID: 40229247 -
Cell Death Dis
Epigenetic silencing of ZIC4 contributes to cancer progression in hepatocellular carcinoma. [Abstract]2020 Oct 23;11(10):906. PMID: 33097694
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Oct 23;11(10):906. [Abstract]
Western blot analysis of EZH2, ZIC4, H3K27me3, and β-actin in HepG2 without or with DZNep (10 μM) treatment for 72 h.
-
J Immunother Cancer
2019 Nov 14;7(1):300. PMID: 31727135 -
J Exp Med
Adenosine metabolic clearance maintains liver homeostasis by licensing arginine methylation of RIPK1. [Abstract]2026 Jan 5;223(1):e20250603. PMID: 41081715
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Med. 2026 Jan 5;223(1):e20250603. [Abstract]
The levels of p-RIPK1(S166), CC8, CC3, and ADK were detected by Western blotting using DZNep (3-Deazaneplanocin A: 10 μM; 12 h).
-
Cell Death Discov
2024 Jul 28;10(1):341. PMID: 39069522 -
J Am Soc Nephrol
The Histone Methyltransferase Enzyme Enhancer of Zeste Homolog 2 Protects against Podocyte Oxidative Stress and Renal Injury in Diabetes. [Abstract]2016 Jul;27(7):2021-34. PMID: 26534922
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2016 Jul;27(7):2021-34. [Abstract]
Immunoblotting mouse podocytes for (A) EZH2 and (B) H3K27me3 under control conditions or after DZNep treatment for 48 hours. Initial immunoblotting experiments confirm the presence of EZH2 protein in cultured mouse podocytes and its depletion with DZNep (A) together with a concurrent reduction in H3K27me3 levels (B).
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2016 Jul;27(7):2021-34. [Abstract]
MEF cells transfected or untransfected with siAdk were stimulated with Flag-TNFα (10 ng/ml) for 15 min, followed by pretreatment with DZNep (3-Deazaneplanocin A: 10 μM), 5-ITu (20 μM), or adenosine (1 mM) for 1 h. Anti-Flag antibody was used to immunoprecipitate complex I, and the levels of RIPK1 R606me2s in complex I or whole-cell lysates were determined by Western blotting.
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2016 Jul;27(7):2021-34. [Abstract]
HEK293T cells were co-transfected with HA-tagged RIPK1-DD and Flag-tagged RIPK1-DD expression plasmids for 24 hours. Cells were then treated with DZNep (3-Deazaneplanocin A: 10 μM), siADK, or adenosine (1 mM). The interaction between Flag-tagged and HA-tagged proteins was detected by immunoprecipitation and Western blotting.
-
Apoptosis
Valproic acid upregulates the expression of the p75NTR/sortilin receptor complex to induce neuronal apoptosis. [Abstract]2020 Oct;25(9-10):697-714. PMID: 32712736 -
Cell Rep
Depletion of CUL4B in macrophages ameliorates diabetic kidney disease via miR-194-5p/ITGA9 axis. [Abstract]2023 May 23;42(6):112550. PMID: 37224018 -
Int Immunopharmacol
EZH2-mediated H3K27me3 promotes autoimmune hepatitis progression by regulating macrophage polarization. [Abstract]2022 May:106:108612. PMID: 35193055 -
J Mol Cell Cardiol
2019 Oct:135:119-133. PMID: 31408621 -
Cancers (Basel)
HDAC2- and EZH2-Mediated Histone Modifications Induce PDK1 Expression through miR-148a Downregulation in Breast Cancer Progression and Adriamycin Resistance. [Abstract]2022 Jul 23;14(15):3600. PMID: 35892859 -
Cell Signal
Enhancer of zeste homolog 2 (EZH2)-dependent sirtuin-3 determines sensitivity to glucose starvation in radioresistant head and neck cancer cells. [Abstract]2024 Mar:115:111029. PMID: 38163576 -
FASEB J
2025 May 15;39(9):e70605. PMID: 40326780 -
J Pharmacol Exp Ther
Downregulation of TrkB Expression and Signaling by Valproic Acid and Other Histone Deacetylase Inhibitors. [Abstract]2019 Sep;370(3):490-503. PMID: 31308194 -
Lab Invest
EZH2 is associated with cartilage degeneration in osteoarthritis by promoting SDC1 expression via histone methylation of the microRNA-138 promoter. [Abstract]2021 May;101(5):600-611. PMID: 33692439 -
Exp Mol Pathol
EGFRvIII epigenetically regulates ARHI to promote glioma cell proliferation and migration. [Abstract]2020 Feb:112:104344. PMID: 31751560 -
AMB Express
SETDB1 knockdown boosts recombinant protein in CHO cells via epigenetic transcriptional silencing. [Abstract]2025 Jul 26;15(1):110. PMID: 40715620 -
Exp Eye Res
Hypoxia-driven histone modification landscape and the role of EZH2 in retinal neovascularization. [Abstract]2025 Sep 26:110670. PMID: 41016422 -
Genes (Basel)
CHIR99021 and Brdu Are Critical in Chicken iPSC Reprogramming via Small-Molecule Screening. [Abstract]2024 Sep 13;15(9):1206. PMID: 39336797 -
Cell Reprogram
Cocktail of Chemical Compounds and Recombinant Proteins Robustly Promote the Stemness of Adipose-Derived Stem Cells. [Abstract]2017 Dec;19(6):363-371. PMID: 29215942 -
Biochem Biophys Res Commun
Down-regulated lncRNA MEG3 promotes osteogenic differentiation of human dental follicle stem cells by epigenetically regulating Wnt pathway. [Abstract]2018 Sep 10;503(3):2061-2067. PMID: 30103943
3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067. [Abstract]
Western blot analysis of H3K27me3, bcatenin and RUNX2 protein accumulation in hDFSCs transfected by EZH2-siRNA and treated with DMSO or DZNep after 3 days of osteogenic induction.
-
Cells Tissues Organs
Targeting EZH2 Ameliorates the LPS-Inhibited PDLSC Osteogenesis via Wnt/β-Catenin Pathway. [Abstract]2020;209(4-6):227-235. PMID: 33461200 -
-
-
-
bioRxiv
2023 Apr 21:2023.04.19.537556. PMID: 37131802 -
-
-
-
Solvent & Solubility
H2O : 50 mg/mL (167.38 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (167.38 mM); Clear solution; Need ultrasonic
Protocol
AML HL-60 cells are obtained and maintained. OCI-AML-3 cells are cultured in α minimum essential medium with 10% fetal bovine serum, and 1% nonessential amino acids. To analyze synergism between 3-Deazaneplanocin A and PS in inducing apoptosis, cells are treated with 3-Deazaneplanocin A (100-750 nM) and PS (5-20 nM) at a constant ratio for 48 hours. The percentage of apoptotic cells is determined by flow cytometry. The combination index (CI) for each drug combination is obtained by median dose effect of Chou and Talalay, using the CI equation within the commercially available software Calcusyn[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
HL-60 cells (5 million) are injected into the tail vein of female nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice, and the mice are monitored for 7 days. The following treatments are administered in cohorts of 7 mice for each treatment: vehicle alone, 1 mg/kg 3-Deazaneplanocin A, 10 mg/kg PS, and 3-Deazaneplanocin A plus PS. Treatments are initiated on day 7. 3-Deazaneplanocin A is administered twice per week (Tuesday-Thursday) intraperitoneally for 2 weeks, and then discontinued. PS is administered 3 days per week (Monday, Wednesday, and Friday) for 4 weeks. The survival of mice from the tail vein model is represented with a Kaplan-Meier survival plot.
Rats[4]
Male wistar rats are used. The acute toxicity study is carried out to determine the NOAEL of 3-Deazaneplanocin A in rats. In total, 20 rats are divided into 4 groups of five each. Three groups are intravenously administered 20, 15, 10 mg/kg body weight (BW) DZNep solution by the tail vein. The remaining group is given physiological saline (0.9% NaCl saline) as the control group. Then, the NOAEL of free DZNep is determined, depending on the following endpoint parameters obtained.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (285 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Handling Instructions (2659 KB)
References
[1]. Fiskus W, et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor LBH589 against human AML cells. Blood, 2009, 114(13), 2733-2743. [Content Brief]
[2]. Avan A, et al. Molecular mechanisms involved in the synergistic interaction of the EZH2 inhibitor 3-deazaneplanocin A with LY 188011 in pancreatic cancer cells. Mol Cancer Ther. 2012 Aug;11(8):1735-46. [Content Brief]
[3]. Kikuchi J, et al. Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells. Lung Cancer. 2012 Nov;78(2):138-43. [Content Brief]
[4]. Sun F, et al. Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus?. Eur J Pharm Sci. 2015 Sep 18;77:290-302. [Content Brief]
[5]. Noriko Uchiyama, et al. Aristeromycin and DZNeP cause growth inhibition of prostate cancer via induction of mir-26a. Eur J Pharmacol. 2017 Oct 5;812:138-146. [Content Brief]
[6]. Robert O Baker, et al. Potential antiviral therapeutics for smallpox, monkeypox and other orthopoxvirus infections. Antiviral Res. 2003 Jan;57(1-2):13-23. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 3.3475 mL | 16.7375 mL | 33.4750 mL | 83.6876 mL |
| 5 mM | 0.6695 mL | 3.3475 mL | 6.6950 mL | 16.7375 mL | |
| 10 mM | 0.3348 mL | 1.6738 mL | 3.3475 mL | 8.3688 mL | |
| 15 mM | 0.2232 mL | 1.1158 mL | 2.2317 mL | 5.5792 mL | |
| 20 mM | 0.1674 mL | 0.8369 mL | 1.6738 mL | 4.1844 mL | |
| 25 mM | 0.1339 mL | 0.6695 mL | 1.3390 mL | 3.3475 mL | |
| 30 mM | 0.1116 mL | 0.5579 mL | 1.1158 mL | 2.7896 mL | |
| 40 mM | 0.0837 mL | 0.4184 mL | 0.8369 mL | 2.0922 mL | |
| 50 mM | 0.0670 mL | 0.3348 mL | 0.6695 mL | 1.6738 mL | |
| 60 mM | 0.0558 mL | 0.2790 mL | 0.5579 mL | 1.3948 mL | |
| 80 mM | 0.0418 mL | 0.2092 mL | 0.4184 mL | 1.0461 mL | |
| 100 mM | 0.0335 mL | 0.1674 mL | 0.3348 mL | 0.8369 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
3-Deazaneplanocin A hydrochloride Related Classifications
HY-12186 Related Classifications
Powered by Bioz