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Chemical Structure| 120964-45-6 Chemical Structure| 120964-45-6

Structure of 3-Deazaneplanocin A HCl
CAS No.: 120964-45-6

Chemical Structure| 120964-45-6

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3-Deazaneplanocin A (DZNep) can inhibit S-adenosine-L-homocysteine hydrolase (AHCY). 3-Deazaneplanocin A HCl is a potent inhibitor of histone methyltransferase EZH2.

Synonyms: DZNep hydrochloride; 3-Deazaneplanocin hydrochloride; 2,3-DMMC

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Product Details of 3-Deazaneplanocin A HCl

CAS No. :120964-45-6
Formula : C12H15ClN4O3
M.W : 298.73
SMILES Code : O[C@@H]1[C@H](O)C(CO)=C[C@H]1N2C=NC3=C2C=CN=C3N.[H]Cl
Synonyms :
DZNep hydrochloride; 3-Deazaneplanocin hydrochloride; 2,3-DMMC
MDL No. :MFCD18782644
InChI Key :UNSKMHKAFPRFTI-FDKLLANESA-N
Pubchem ID :14563109

Safety of 3-Deazaneplanocin A HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of 3-Deazaneplanocin A HCl

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    S-adenosylhomocysteine hydrolase, Ki:50 pM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human retinal endothelial cells 5 µM 4 days Inhibition of Ezh2 reduced H3K27me3 levels and Ezh2 recruitment at the MMP-9 promoter, thereby decreasing MMP-9 expression and activity. PMC5737805
OM-induced tumor spheroids 0.5, 1, 2.5, 5 µM 1-3 days Ezh2 inhibition blocked OM-induced cancer cell growth, and DZNep reduced the size of ex vivo cultures of OM-derived tumor spheroids. PMC6989674
KMCH cells 1 μM 2 days To inhibit EZH2 activity and observe its effect on the expression of c-Myc, MafG, and c-Maf. Results showed that inhibiting EZH2 increased the expression of c-Myc, MafG, c-Maf, and MAT1A, but did not prevent MAT1A overexpression from lowering their mRNA levels. PMC4956551
DU145 cells 2.5 μM or 5 μM 2 or 3 days To evaluate the de-repression effect of DZNep on PRC2-targeted miRNAs, results showed increased expression of miR-181a,b, miR-200a,b,c, and miR-203, while control miRNAs miR-217, miR-219, and miR-21 were unaffected. PMC3157014

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Subcutaneous transplantation model Subcutaneous injection 100 μg/kg Every 3 days for 6 weeks To evaluate the effect of DZNep on the osteogenic capacity of aged BMSCs in vivo, results showed that DZNep significantly restored the osteogenic capacity of aged BMSCs. PMC8743666

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.33mL

16.74mL

3.35mL

1.67mL

33.48mL

6.70mL

3.35mL

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