3-Deazaneplanocin A

SKU: orb1908993

Description

3-Deazaneplanocin A (DZNep) is a dual inhibitor of EZH2 and AHCY, promoting target degradation via the proteasome. It exhibits antifibrotic activity in hepatic, renal, and pulmonary models and has been studied in both cellular assays and animal models of fibrosis.

Research Area

Epigenetics & Chromatin, Infectious Disease & Virology

Key Properties

• CAS Number: 102052-95-9
• MW: 262.27
• Purity: 99.68% (May vary between batches)
• Formula: C₁₂H₁₄N₄O₃
• SMILES: O[C@H]1[C@H](N2C=3C(N=C2)=C(N)N=CC3)C=C(CO)[C@H]1O
• Target: Virus Protease,Histone Methyltransferase
• Solubility: DMSO:75 mM;H2O:80 mg/mL (305.03 mM)

Bioactivity

• Target IC50:
  NSCLC:0.08 to 0.24 μM|MIAPaCa2 cells:1 μM
• 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. 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.
• 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. 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. 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.

Storage & Handling

• 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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

3 Deazaneplanocin A, 3-Deazaneplanocin, 3Deazaneplanocin A, 3-Deazaneplanocin A, DZNep, Orthopoxvirus, Histone Methyltransferase, HistoneMethyltransferase, EZH2

Compound Identifiers

PubChem CID

73087