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3-Deazaneplanocin A
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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
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $159 | In Stock | |
| 5 mg | $427 | 7-10 days |
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Purity:99.68%
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Product Introduction
Bioactivity
Chemical Properties
| 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 | MIAPaCa2 cells:1 μM, non-small cell lung cancer (NSCLC) cell lines:0.08 to 0.24 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] |
| Alias | DZNep, 3-Deazaneplanocin |
| 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. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 75 mM H2O: 80.00 mg/mL (305.03 mM), Sonication is recommended | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/H2O
H2O
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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