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3-Deazaneplanocin A

Name: 3-Deazaneplanocin A
Brand: TargetMol
SKU: T6292
Price: 129 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6292Cas No. 102052-95-9

Alias DZNep, 3-Deazaneplanocin

3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.

3-Deazaneplanocin A

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Purity: 99.68%

Catalog No. T6292Alias DZNep, 3-DeazaneplanocinCas No. 102052-95-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$129	In Stock	In Stock
5 mg	$353	In Stock	In Stock
10 mg	$525	-	In Stock
25 mg	$843	-	In Stock
50 mg	$1,130	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.68%

Appearance:Solid

Color:White

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COA

Product Introduction

Bioactivity

Description	3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.
Targets&IC50	NSCLC:0.08 to 0.24 μM, MIAPaCa2 cells:1 μM
In vitro	Under 1.0 μM 3-Deazaneplanocin A (DZNep) treatment, OCI-AML3 cells showed an increase in cell number at G0/G1 phase, indicating cell cycle arrest. 3-Deazaneplanocin A treatment for 48 hours was able to dose-dependently inhibit the colony-forming ability of OCI-AML3 and HL-60 cells in the concentration range of 200 nM to 2.0 μM. [1] In addition, 3-Deazaneplanocin A treatment for 72 hours significantly reduced the expression of EZH2 in several cancer cell lines (e.g., PANC-1, MIA-PaCa-2, and LPc006) by 48%, 32%, and 36%, respectively. Although 3-Deazaneplanocin A had a weak inhibitory effect on the proliferation of PANC-1 cells, it had a stronger inhibitory effect on MIA-PaCa-2 and LPc006 cells, with IC50 values of 1 μM and 0.1 μM, respectively.[2] In non-small cell lung cancer (NSCLC) cell lines, 3-Deazaneplanocin A also exhibited dose-dependent inhibition of proliferation with IC50 ranging from 0.08 to 0.24 μM.[3]
In vivo	In the NOD/SCID mouse model, the median survival of acute myeloid leukemia (AML) mice was significantly prolonged in the treatment group with the combination of 3-Deazaneplanocin A and Panobinostat (PS) compared to the group with the drug alone and the control group. Specifically, 36 days for the control group, 42 days for PS, 43 days for 3-Deazaneplanocin A, and 52 days for the combination group. [1] In addition, administration of 20 mg/kg 3-Deazaneplanocin A to rats significantly reduced body weight during the first three days of treatment (2.0%, 4.9%, and 1.2% reductions, respectively), and suppressed the rate of body weight growth to 2.6% per day from the fourth day on. [4]
Synonyms	DZNep, 3-Deazaneplanocin

Chemical Properties

Molecular Weight	262.27
Formula	C₁₂H₁₄N₄O₃
Cas No.	102052-95-9
Smiles	O[C@H]1[C@H](N2C=3C(N=C2)=C(N)N=CC3)C=C(CO)[C@H]1O
Relative Density.	1.75 g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 75 mM, Sonication is recommended.

H2O: 80 mg/mL (305.03 mM), Sonication is recommended.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	3.8129 mL	19.0643 mL	38.1286 mL	190.6432 mL
5 mM	0.7626 mL	3.8129 mL	7.6257 mL	38.1286 mL
10 mM	0.3813 mL	1.9064 mL	3.8129 mL	19.0643 mL
20 mM	0.1906 mL	0.9532 mL	1.9064 mL	9.5322 mL
50 mM	0.0763 mL	0.3813 mL	0.7626 mL	3.8129 mL

H2O

	1mg	5mg	10mg	50mg
100 mM	0.0381 mL	0.1906 mL	0.3813 mL	1.9064 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc