GSK4418959

SKU: orb2945994

Description

GSK4418959 (IDE275) is an orally bioavailable, selective, and reversible ATP-competitive inhibitor of Werner syndrome helicase (WRN). It potently blocks WRN's ATPase and helicase activities, serving as a key research tool for investigating WRN's essential role in MSI-H cancer models, both in cellular and in vivo studies.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 3064599-36-3
• MW: 646.65
• Purity: 99.14% (May vary between batches)
• Formula: C₃₁H₃₀F₄N₄O₅S
• SMILES: C(O)(=O)[C@@H]1[C@H](CCC[C@H]1C(NC2=C(F)C=C(C(F)(F)F)C=C2)=O)C3=CC=C(N(S(=O)(=O)C=4C=C5C(=CC4)N(C)C(C)=N5)C)C=C3
• Target: DNA/RNA Synthesis
• Solubility: DMSO:80 mg/mL (123.71 mM)

Bioactivity

• In Vivo:
  GSK4418959 (IDE275) induces tumor regression and activates DNA damage response (DDR) markers in several MSI-H CDX and PDX models across diverse tumor types, including CRC, endometrial, and gastric cancers with varying oncogenic drivers and tumor suppressor mutations, while sparing MSS models.
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Storage & Handling

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

Alternative Names

IDE 275, IDE275, GSK 4418959

Compound Identifiers

PubChem CID

172618374