PARP-1-IN-2

SKU: orb2900806

Description

PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.

Key Properties

• CAS Number: 684234-55-7
• MW: 424.28
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₅Cl₂N₃O₂
• SMILES: Clc1ccc(cc1)-c1nn(CC(=O)Nc2cccc(Cl)c2)c(=O)c2ccccc12
• Target: PARP
• Solubility: In Vitro: DMSO : 83.33 mg/mL (196.40 mM; Ultrasonic )

Bioactivity

• In Vitro:
  PARP-1-IN-2 (compound 11 g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells. PARP-1-IN-2 (0-10 μM, 24 h) decreases the expression of pro-caspase-3 and phosphorylated AKT, increases the expression of caspase-3, caspase-9 protein and the cleaved PARP-1.Cell Proliferation Assay Cell line: A549, HFF cells. Concentration: 0, 0.1, 1, 10 μM Incubation time: 24, 48 h. Result: Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells. Western blot analysis. Cell line: A549 cells. Concentration: 0, 0.1, 1, 10 μM Incubation time: 24 h. Result: Reduced expression of pro-caspase-3 and phosphorylated AKT, significantly increased the expression of caspase-3 and caspase-9 protein, and enhanced expression of the cleaved PARP-1.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PARP