PARP-1-IN-3

SKU: orb1944639

Description

PARP-1-IN-3 is a highly potent dual inhibitor of PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively. It exhibits anti-inflammatory and anticancer properties by inducing apoptosis, causing G2/M cell cycle arrest, and is a valuable tool for in vitro and in vivo cancer research.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 2976342-33-1
• MW: 425.28
• Purity: 98.38% (May vary between batches)
• Formula: C₂₁H₁₇BrN₂O₃
• SMILES: O=C(N)C=1C=CC=CC1OCC=2C=CC=C(C2)NC(=O)C3=CC=C(Br)C=C3
• Target: PARP|||Apoptosis
• Solubility: DMSO:100 mg/mL (235.14 mM)

Bioactivity

• Target IC50:
  NCM460 cells:486.87 μM|PARP2:2.34 nM|PARP1:0.25 nM|SW480 cells:33.69 μM|DLD-1 cells:2.83 μM|HCT116 cells:0.30 μM
• In Vitro:
  PARP-1-IN-3 (compound 13f) demonstrates effective anticancer activity with IC50 values of 0.30 μM, 2.83 μM, 33.69 μM, and 486.87 μM against HCT116, DLD-1, SW480, and NCM460 cells, respectively, following a 48-hour treatment. In HCT116 cells, PARP-1-IN-3 (0.3-3 μM) inhibits colony formation and migration over 24-48 hours. A 48-hour treatment with PARP-1-IN-3 (0.3-3 μM) induces the accumulation of DNA double-strand breaks in HCT116 cells. Treatment with PARP-1-IN-3 (0.3-7.5 μM) for 48-72 hours results in cell cycle arrest at the G2/M phase, reduced mitochondrial membrane potential, and apoptosis in HCT116 cells.
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Storage & Handling

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

Alternative Names

PARP1, Apoptosis

Compound Identifiers

PubChem CID

168355539