3-Deazaneplanocin A (Synonyms: DZNep; 3-Deazaneplanocin)

Cat. No.: HY-10442: FAQs
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3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (3-Deazaneplanocin A hydrochloride) that retains the same biological activity.

For research use only. We do not sell to patients.

3-Deazaneplanocin A Chemical Structure

CAS No. : 102052-95-9

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Other In-stock Forms of 3-Deazaneplanocin A:

3-Deazaneplanocin A hydrochloride

Other Forms of 3-Deazaneplanocin A:

3-Deazaneplanocin A hydrochloride In-stock

26 Publications Citing Use of MCE 3-Deazaneplanocin A

: 3-Deazaneplanocin A 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.

: 3-Deazaneplanocin A 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.

: 3-Deazaneplanocin A 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).

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor^[1]^[2]. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity^[6]^[7].

IC₅₀ & Target

EZH2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.4 μM Compound: 4	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay	[PMID: 26010585]
HCT-116	IC₅₀	0.26 μM Compound: 4	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay	[PMID: 26010585]
MDA-MB-231	IC₅₀	0.3 μM Compound: 4	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay	[PMID: 26010585]
PC-3	IC₅₀	9.39 μM Compound: 4	Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay	[PMID: 26010585]
SK-HEP1	IC₅₀	0.72 μM Compound: 4	Cytotoxicity against human SKHEP1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay Cytotoxicity against human SKHEP1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay	[PMID: 26010585]
SNU-638	IC₅₀	0.91 μM Compound: 4	Cytotoxicity against human SNU638 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay Cytotoxicity against human SNU638 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay	[PMID: 26010585]
Vero	IC₅₀	> 500 μg/mL Compound: 2	Cytotoxic effect on host cells during stationary phase of virus in vero cell cultures using MTT method Cytotoxic effect on host cells during stationary phase of virus in vero cell cultures using MTT method	10.1016/S0960-894X(01)80163-3
Vero	IC₅₀	0.55 μg/mL Compound: 2	Cytotoxic effect on host cells during growth phase of virus in vero cell cultures using MTT method Cytotoxic effect on host cells during growth phase of virus in vero cell cultures using MTT method	10.1016/S0960-894X(01)80163-3

In Vitro

3-Deazaneplanocin A 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 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 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±0.3 and 0.1±0.03 μM, respectively^[2]. 3-Deazaneplanocin A 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.

In Vivo

The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A and Panobinostat (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days^[1]. There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day). Administration of 20 mg/kg 3-Deazaneplanocin A not only markedly reduces the relative weight of the rats compare to the initial weight (?2.0%, ?4.9% and ?1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

262.26

Formula

C₁₂H₁₄N₄O₃

CAS No.

102052-95-9

Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@H](O)C(CO)=C[C@H]1N2C=NC3=C2C=CN=C3N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (381.30 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.8130 mL	19.0650 mL	38.1301 mL
5 mM	0.7626 mL	3.8130 mL	7.6260 mL
10 mM	0.3813 mL	1.9065 mL	3.8130 mL

View the 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. 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

3-Deazaneplanocin A (DZNep) is prepared in PBS^[5].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (255 KB) HNMR (257 KB) RP-HPLC (184 KB) MS (68 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 panobinostat 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 gemcitabine 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]. Siddiqi FS, et al. The Histone Methyltransferase Enzyme Enhancer of Zeste Homolog 2 Protects against Podocyte Oxidative Stress and Renal Injury in Diabetes. J Am Soc Nephrol. 2016 Jul;27(7):2021-34. [Content Brief]

[6]. 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]

[7]. Smee DF, et al. A review of compounds exhibiting anti-orthopoxvirus activity in animal models. Antiviral Res. 2003 Jan;57(1-2):41-52. [Content Brief]

Cell Assay ^[1]	AML HL-60 cells are obtained and maintained. OCI-AML-3 cells are cultured in α minimum essential medium with 10% fetal bovine serum, 1% penicillin/streptomycin, 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[4]	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) 3-Deazaneplanocin A 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 3-Deazaneplanocin A is determined, depending on the following endpoint parameters obtained. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Fiskus W, 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, 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 gemcitabine 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]. Siddiqi FS, et al. The Histone Methyltransferase Enzyme Enhancer of Zeste Homolog 2 Protects against Podocyte Oxidative Stress and Renal Injury in Diabetes. J Am Soc Nephrol. 2016 Jul;27(7):2021-34. [Content Brief] [6]. 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] [7]. Smee DF, et al. A review of compounds exhibiting anti-orthopoxvirus activity in animal models. Antiviral Res. 2003 Jan;57(1-2):41-52. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.8130 mL	19.0650 mL	38.1301 mL	95.3252 mL
	5 mM	0.7626 mL	3.8130 mL	7.6260 mL	19.0650 mL
	10 mM	0.3813 mL	1.9065 mL	3.8130 mL	9.5325 mL
	15 mM	0.2542 mL	1.2710 mL	2.5420 mL	6.3550 mL
	20 mM	0.1907 mL	0.9533 mL	1.9065 mL	4.7663 mL
	25 mM	0.1525 mL	0.7626 mL	1.5252 mL	3.8130 mL
	30 mM	0.1271 mL	0.6355 mL	1.2710 mL	3.1775 mL
	40 mM	0.0953 mL	0.4766 mL	0.9533 mL	2.3831 mL
	50 mM	0.0763 mL	0.3813 mL	0.7626 mL	1.9065 mL
	60 mM	0.0636 mL	0.3178 mL	0.6355 mL	1.5888 mL
	80 mM	0.0477 mL	0.2383 mL	0.4766 mL	1.1916 mL
	100 mM	0.0381 mL	0.1907 mL	0.3813 mL	0.9533 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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

3-Deazaneplanocin A102052-95-9DZNep 3-DeazaneplanocinHistone MethyltransferaseOrthopoxvirusInhibitorinhibitorinhibit

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3-Deazaneplanocin A (Synonyms: DZNep; 3-Deazaneplanocin)

Other Forms of 3-Deazaneplanocin A:

3-Deazaneplanocin A Related Antibodies

26 Publications Citing Use of MCE 3-Deazaneplanocin A

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

3-Deazaneplanocin A Related Antibodies

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Complete Stock Solution Preparation Table

3-Deazaneplanocin A Related Classifications

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