GSK4418959

GSK4418959 (IDE275) is a selective, reversible and orally active WRN helicase inhibitor. GSK4418959 shows >10,000-fold selectivity over other helicases. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer, such as colorectal cancer (CRC) and endometrial cancer (EC) [1].

Product Specifications

CAS Number

[3064599-36-3]

Product Name Alternative

IDE275

UNSPSC

12352005

Target

DNA/RNA Synthesis

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/wrn-inhibitor-16.html

Concentration

10mM

Purity

99.07

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=C(C(F)(F)F)C=C1F)[C@@H]2CCC[C@H](C3=CC=C(N(C)S(=O)(C4=CC(N=C(C)N5C)=C5C=C4)=O)C=C3)[C@H]2C(O)=O

Molecular Formula

C31H30F4N4O5S

Molecular Weight

646.65

References & Citations

[1]Yanhua Rao, et al. Abstract 6393: Patient selection, target engagement and pharmacodynamic markers of WRN inhibitor GSK4418959 (IDE275) . Cancer Res (2025) 85 (8_Supplement_1) : 6393.|[2]Joshua P. Taygerly, et al. Abstract 5750: Discovery of GSK4418959 (IDE275) : A novel, non-covalent, reversible Werner Helicase inhibitor and a new potential therapeutic for the treatment of MSI-H cancers. Cancer Res (2025) 85 (8_Supplement_1) : 5750.