APE1-IN-1

SKU: orb1688548

Description

APE1-IN-1 is a potent, brain-penetrant inhibitor of the AP endonuclease 1 (APE1) protein. It demonstrates antitumor potential and, in vitro, synergistically enhances the cell-killing effects of alkylating agents like methyl methanesulfonate in cancer research.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 524708-03-0
• MW: 371.52
• Purity: 98.50% (May vary between batches)
• Formula: C₁₉H₂₁N₃OS₂
• SMILES: CC(C)N1CCc2c(C1)sc(NC(C)=O)c2-c1nc2ccccc2s1
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.69 mM);DMSO:10 mg/mL (26.92 mM)

Bioactivity

• Target IC50:
  qHTS assay:2 μM|Radiotracer incision assay:12 μM
• In Vivo:
  Administered at a single dosage of 30 mpk via intraperitoneal injection, APE1-IN-1 demonstrates favorable pharmacokinetic properties.
• In Vitro:
  In the qHTS assay, APE1-IN-1 (compound 3) displays an IC50 of 2 μM, while in a radiotracer incision assay (RIA), it exhibits an IC50 of 12 μM. In a dose-dependent manner, APE1-IN-1 (at concentrations of 0, 1, 3, 10, 30, or 100 μM for 15 minutes) inhibits AP site incision in HeLa whole cell extracts. Furthermore, APE1-IN-1 (at concentrations ranging from 5 to 30 μM for 24 hours) demonstrates cytotoxic activity against HeLa cells and enhances the activity of methyl methansulfonate and Temozolomide.
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Storage & Handling

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

Alternative Names

DNA Synthesis, DNASynthesis, APE1, RNASynthesis, RNA Synthesis

Compound Identifiers

PubChem CID

3581333