3-Deazaneplanocin,DZNep (Synonyms: DZNep, NSC 617989) |
| رقم الكتالوجGC13145 |
An inhibitor of lysine methyltransferase EZH2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 102052-95-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
3-Deazaneplanocin is a highly potent inhibitor of S-adenosylhomocysteine hydrolase with Ki value of 0.05 nM [1].
3-Deazaneplanocin was synthesized as an inhibitor of S-adenosylhomocysteine hydrolase. It is an analog of adenosine and inhibits S-adenosylhomocysteine hydrolase through competing with the substrate, adenosine. 3-Deazaneplanocin was not so that potent in cell growth inhibition. 10 μM 3-Deazaneplanocin treatment resulted in moderate cell growth reduction in HL-60 cells. In HCC cell lines Huh1 and Huh7, 3-Deazaneplanocin inhibited growth and non-adherent sphere formation dose-dependently. It decreased the epithelial cell adhesion molecule EpCAMhigh fraction from 49.0% to 12.5% in Huh1 cells and from 44.4% to 11.6% in Huh7 cells. Moreover, in mice implanted with Huh7 cells, administration of 3-Deazaneplanocin suppressed tumor initiation and growth via directly affecting the growth and self-renewal of tumor-initiating cells [1, 2].
References:
[1] Glazer R I, Hartman K D, Knode M C, et al. 3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochemical and biophysical research communications, 1986, 135(2): 688-694.
[2] Chiba T, Suzuki E, Negishi M, et al. 3-Deazaneplanocin A is a promising therapeutic agent for the eradication of tumor-initiating hepatocellular carcinoma cells. International Journal of Cancer, 2012, 130(11): 2557-2567.
| Cell experiment:[1] | |
|
Cell lines |
Human acute myeloid leukemia (AML) cell |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
100-750 nM; 24-72h |
|
Applications |
DZNep induced apoptosis in cultured and primary AML cells. DZNep exhausted EZH2 levels, and inhibits trimethylation of lysine 27 on histone H3 in the AML HL-60 and OCI-AML3 cells. DZNep induced the levels of p16, p21, p27, and FBXO32 after cyclin E and HOXA9 levels run out. |
| Animal experiment:[2] | |
|
Animal models
|
Sprague-Dawley rats (120–140 g) |
|
Dosage form
|
5μM DZNep for 24 h pre-treatment before experiment, orally taken with diets |
|
Applications |
DZNep significantly reduced EZH2 expression and activity, and it increased lipid accumulation, inflammatory molecules and microRNAs in non-alcoholic fatty liver disease (NAFLD) mouse model. |
|
Other notes
|
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: 1. Fiskus W1, Wang Y, Sreekumar A 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 Sep 24;114(13):2733-43. 2. Vella S, Gnani D, Crudele A et al. EZH2 down-regulation exacerbates lipid accumulation and inflammation in vitro and in vivo NAFLD.Int J Mol Sci. 2013 Dec 12;14(12):24154-68. |
|
| Cas No. | 102052-95-9 | SDF | |
| المرادفات | DZNep, NSC 617989 | ||
| Chemical Name | (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol | ||
| Canonical SMILES | C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N | ||
| Formula | C12H24N4O3 | M.Wt | 262.26 |
| الذوبان | DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.813 mL | 19.065 mL | 38.1301 mL |
| 5 mM | 0.7626 mL | 3.813 mL | 7.626 mL |
| 10 mM | 0.3813 mL | 1.9065 mL | 3.813 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *