PJ34

SKU: orb1300989

Description

PJ34

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 344458-19-1
• MW: 295.34
• Purity: 99.85%
• Formula: C₁₇H₁₇N₃O₂
• SMILES: CN(C)CC(=O)Nc1ccc2[nH]c(=O)c3ccccc3c2c1
• Target: PARP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.39 mM);DMSO:2.96 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  PARP2:86 nM|PARP1:110 nM|PARP:20 nM (EC50)
• In Vivo:
  To assess PJ34's comparative potency and efficacy against other PARP inhibitors, it was tested at 3.2 and 10 mg/kg doses. The 3.2 mg/kg dose significantly decreased cortical damage by 33%, whereas the 10 mg/kg dose showed a reversed effect, reducing damage by only 17%. Furthermore, a 25 mg/kg dose of PJ34 significantly lowered TNF-α mRNA levels in ischemic animals by 70%, aligning these levels with those found in sham or naive animals. Additionally, this treatment notably diminished E-selectin and ICAM-1 mRNA levels by 81% and 54%, respectively, in ischemic mice compared to those treated with a vehicle.
• In Vitro:
  PJ34 effectively inhibits PARP enzyme activity, exhibiting an IC50 of 110±1.9 nM. Its neuroprotective properties are assessed in PC12 cells through LDH assay, comparing favorably with other PARP inhibitors. Additionally, PJ34 treatment significantly reduces cell death in a concentration-dependent manner, within the range of 10-7 to 10-5 M.
• Cell Research:
  PJ34 is dissolved in 100% DMSO at 10 mM and then diluted in DMEM without serum. PC12 cell cultured are grown in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 5% (v/v) horse serum, and a 1% (v/v) penicillin-streptomycin antibiotics mixture. Cells are grown in an atmosphere of 95% air and 5% CO2 at 37°C. For all experiment, cells are seeded at a density of 4×104 cells/well in 96-well culture plates and allowed to attach overnight. For assessment of cell viability, hydrogen peroxide-induced cytotoxicity is quantified by a standard measurement of LDH release with the use of the LDH assay kit. Briefly, 6 h after hydrogen peroxide exposure, 20 μL of medium of each well is collected, and the solution prepared from LDH assay kit is added. After incubation at room temperature for 30 min, the reaction is stopped by addition of 1 N HCl, and absorbance is measured at 450 nm using a microplate reader.

Storage & Handling

• Storage: 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

inhibit, Inhibitor, PARP, PARP1, PARP2, poly ADP ribose polymerase, PJ34, PJ-34, PJ 34

Compound Identifiers

PubChem CID

4858