ERCC1-XPF-IN-2

SKU: orb1689129

Description

ERCC1-XPF-IN-2 is a potent small molecule inhibitor of the ERCC1-XPF endonuclease, exhibiting an IC50 of 0.6 μM. It is active in nucleotide excision repair and cisplatin enhancement assays, and its utility in DNA damage response research is supported by activity in γH2AX-based cellular models.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1808986-37-9
• MW: 326.17
• Purity: 98.21% (May vary between batches)
• Formula: C₁₅H₁₃Cl₂NO₃
• SMILES: Oc1ccc(CNC(=O)Cc2ccc(Cl)cc2Cl)cc1O
• Target: Others,DNA/RNA Synthesis
• Solubility: DMSO:225 mg/mL (689.82 mM)

Bioactivity

• In Vitro:
  ERCC1-XPF-IN-2 (compound 13) (0-100 µM) exhibits DNase I and FEN-1 activity with IC50s of >100 µM, and shows binding kinetics with a Kd of ~30 µM. It is non-toxic to Hep-G2 cells at 10 µM and has short microsomal half-lives in mouse (23 min) and human (28 min). At 0-60 µM for 24 hours, it inhibits nucleotide excision repair (NER) with an IC50 of 15.6 µM in A375 cells and enhances cisplatin activity without toxicity. Additionally, at 10 µM for 6 hours, it delays DNA repair, indicated by an increase in γH2AX foci per cell.
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Storage & Handling

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

Alternative Names

endonuclease

Compound Identifiers

PubChem CID

122189958