GSK_WRN4

SKU: orb2665293

Description

GSK_WRN4 is a small molecule inhibitor of the WRN helicase, which exhibits anticancer properties by inducing DNA double-strand breaks. It is a valuable research tool for studying DNA damage response and has demonstrated efficacy in inhibiting the growth of MSI-high tumor cells in vitro.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 2923008-66-4
• MW: 336.41
• Formula: C₁₆H₂₀N₂O₄S
• SMILES: O=C1NC(=CC=C1C(N[C@@H]2C=CS(=O)(=O)C2)=O)C3CCCCC3
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (9.81 mM);DMSO:80 mg/mL (237.81 mM)

Bioactivity

• Target IC50:
  WRN helicase:7.6 (pIC50)
• In Vivo:
  In a xenografted mouse model of colorectal cancer cell lines, dose-dependent tumor growth inhibition was observed by oral administration of GSK_WRN4 (30, 100, 300 mpk), and tumor growth was completely inhibited at the highest dose supported by favorable pharmacokinetics. Morphological and pathological analysis of explants showed that GSK_WRN4 treatment resulted in a decrease in SW48 tumor cell density, accompanied by increased stromal and extracellular matrix deposition.
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• In Vitro:
  GSK_WRN4 significantly inhibited WRN helicase activity with pIC50 value of 7.6. GSK_WRN4 (0.1-20 μM, 1.5-144h) treated SW48 cells in a time - and dose-dependent manner.
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Storage & Handling

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

Alternative Names

DNASynthesis, DNA Synthesis, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

172636055