unwinding

ML216 (CID-49852229) is a small molecule inhibitor of BLM helicase with an IC50 of 1.8 μM, demonstrating 28-fold selectivity against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s > 50 μM).

ATPγS tetralithium salt is a good substrate for RNA-stimulated nucleotide hydrolysis and RNA unwinding activity of eIF4A.

Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) keeps DNA from unwinding by inhibiting topoisomerase 1.

GSK4418959 (IDE275) is a non-covalent, reversible, selective, and orally active inhibitor of the Werner syndrome helicase (WRN helicase). GSK4418959 inhibits both ATPase and DNA unwinding activities of WRN helicase in an ATP-competitive manner. GSK4418959 is a valuable chemical tool for the study of microsatellite instability-high (MSI-H) cancers, where WRN helicase plays an essential role in maintaining genomic stability.

WRN-IN-19 (Compound (S)-27) is a covalent WRN helicase inhibitor, with a pIC50 of 5.4 at 0 hours and 7.5 at 4 hours in a DNA-unwinding endpoint assay. It demonstrates synthetic lethality against MSI-H (high microsatellite instability) cancer cells.

HSV-1/HSV-2-IN-3 inhibits the helicase-primase complex of herpes simplex virus (HSV), interfering with the crucial processes of DNA unwinding and primer synthesis necessary for viral genome replication. In gD immunofluorescence assays containing 2% FBS, its EC50 against HSV-2 is 7.0 nM, while in assays with 10% human serum, the EC50 is 57.5 nM. Within qPCR replication analysis, the compound demonstrates an EC50 of 1.1 nM. Additionally, HSV-1/HSV-2-IN-3 exhibits strong selectivity against off-target interactions with human carbonic anhydrase (IC50 for hCA II ≈ 2.9 µM, and > 35 µM for hCA I). This compound is applicable in anti-HSV research.

GSK4418959 enantiomer is the enantiomer of GSK4418959. GSK4418959 (IDE275) is a non-covalent, reversible, selective helicase inhibitor of WRN with oral bioavailability. It competitively inhibits ATPase and DNA unwinding functions in an ATP-dependent manner. GSK4418959 is utilized in the study of microsatellite instability-high (MSI-H) cancer.