Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Helicase inhibitors act on the enzymes that unwind DNA and RNA duplexes during replication and repair. Helicases use adenosine triphosphate (ATP) to separate nucleic acid strands, which gives repair and recombination machinery access to single strands. Cancer cells with microsatellite instability were found in 2019 to depend on the Werner syndrome helicase (WRN), and expanded thymine-adenine (TA) dinucleotide repeats were later linked to that dependence. The list reflects this focus with WRN inhibitors such as VVD-214 and NSC 617145. Related RecQ family enzymes are covered by BLM-IN-2 against the Bloom syndrome helicase (BLM) and by RECQL5-IN-1. DHX9-IN-1 acts on the RNA helicase DExH-box helicase 9 (DHX9), which resolves R-loops and other structured nucleic acids.
BLM-IN-2 is an inhibitor of Bloom's Syndrome Protein (BLM), exhibiting an IC50 value of 0.8 μM. This compound effectively inhibits proliferation, invasion, and induces cell cycle arrest and apoptosis in colorectal cancer (CRC) cells. BLM-IN-2 is a valuable tool for investigating the role of BLM in CRC research and therapeutic strategies.
WRN Inhibitor 2 is a selective inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN). It exhibits a potent inhibition profile with a pIC50 value of 7.0 or higher. This compound is valuable for research into DNA replication and repair mechanisms, particularly in studies related to aging and cancer biology.
Synonyms: RO7589831; VVD-133214
VVD-214 is a synthetic lethal allosteric inhibitor targeting WRN helicase, exhibiting an IC50 of 0.1316 µM. This compound covalently binds to cysteine 727 of WRN, effectively inhibiting ATP hydrolysis and helicase activity. VVD-214 induces double-stranded DNA breaks, nuclear swelling, and cell death, demonstrating significant potential in research focused on high microsatellite instability (MSI) cancers.
NSC 617145 is a selective inhibitor of the Werner syndrome helicase (WRN), exhibiting an IC50 value of 230 nM. This compound effectively inhibits WRN ATPase activity, leading to the induction of double-strand breaks (DSB) and chromosomal abnormalities. NSC 617145 demonstrates a preferred selectivity for WRN compared to other helicases such as BLM, FANCJ, ChlR1, RecQ, and UvrD, making it a valuable tool for investigating the cellular mechanisms of DNA repair and associated diseases.
DHX9-IN-1 is an inhibitor of the ATP-dependent RNA helicase A (DHX9), with an EC50 value of 1.41 μM. This compound exhibits anti-tumor activity, making it a valuable tool for research focused on colorectal cancer and related malignancies. Its mechanism of action allows for the investigation of DHX9's role in cancer progression and potential therapeutic strategies.
Synonyms: IDE275
GSK4418959 is a selective and reversible inhibitor of the WRN helicase, exhibiting over 10,000-fold selectivity compared to other helicases. It functions as an ATP-competitive inhibitor, effectively disrupting ATPase activity and DNA unwinding processes. This compound is particularly relevant for research focused on microsatellite instability-high (MSI-H) cancers, including colorectal cancer (CRC) and endometrial cancer (EC).
RECQL5-IN-1 is a potent inhibitor of RECQL5, targeting both its enzymatic and nonenzymatic domains. This compound demonstrates strong inhibition of RECQL5 helicase activity with an IC50 of 46.3 nM, stabilizing the interaction between RECQL5 and RAD51 proteins. By promoting RAD51 aggregation and inhibiting homologous recombination repair (HRR), RECQL5-IN-1 shows selective cytotoxicity in cancer cells that express RECQL5, making it a valuable tool for cancer research and therapeutic investigations.
DHX9-IN-3 is a potent inhibitor of the ATP-dependent RNA helicase A (DHX9). With an IC50 of 8.7 nM, DHX9-IN-3 effectively inhibits cellular proliferation in LS411N cancer cells. This compound serves as a valuable tool for researchers investigating the role of DHX9 in cancer biology and therapeutic interventions.
H3B-968 is an ATP-competitive inhibitor of Werner syndrome protein (WRN), exhibiting an IC50 of approximately 10 nM. This compound effectively impedes the helicase activity of WRN, making it a valuable tool in research focused on DNA repair mechanisms and cellular aging. H3B-968 is applicable in studies related to genomic stability and the development of therapeutic strategies for disorders associated with WRN dysfunction.
GSK_WRN3 is a selective inhibitor of the WRN helicase, exhibiting an pIC50 of 8.6. It demonstrates potent activity against microsatellite unstable (MSI) cancer cells, effectively inducing DNA damage and leading to cell cycle arrest. GSK_WRN3's anti-tumor properties make it a valuable tool for research in cancer therapy and the study of DNA repair mechanisms.
GSK_WRN4 is a potent WRN helicase inhibitor, exhibiting an approximate pIC50 of 7.6. This compound effectively induces DNA damage markers such as p21, p-γH2AX, and p-KAP1. GSK_WRN4 demonstrates selective inhibition of microsatellite-unstable tumors both in vitro and in vivo, primarily by inducing DNA double-strand breaks, particularly at expanded TA repeats and other damaged DNA regions. This makes it a valuable tool for research into cancer therapeutics and the effects of DNA repair mechanisms.
DHX9-IN-9 is a selective inhibitor of the RNA helicase DHX9, displaying an effective concentration (EC50) of 0.0177 μM in cellular assays. This compound plays a vital role in cancer research by modulating the activity of DHX9, which is implicated in various oncogenic processes. DHX9-IN-9 can be employed to investigate the biological functions of DHX9 and its potential as a therapeutic target in cancer treatment.
WRN Inhibitor 3 is a potent inhibitor of the Werner Syndrome ATP-dependent helicase (WRN), which plays a crucial role in DNA replication and repair. This cyclic vinyl sulfone compound demonstrates significant biological activity in disrupting WRN's function, making it a valuable tool for cancer research. Its application extends to studying the mechanisms of DNA repair pathways and potential therapeutic strategies targeting WRN in various malignancies.
WRN Inhibitor 5 is a cyclic vinyl sulfone compound that selectively inhibits the Werner Syndrome ATP-dependent helicase (WRN). This inhibitor is crucial for studying cancer, particularly in contexts involving microsatellite instability (MSI) and defective DNA mismatch repair (dMMR) mechanisms. Its ability to target WRN provides valuable insights into the molecular underpinnings of certain cancer types and aids in the development of therapeutic strategies.
DHX9-IN-5 is a potent inhibitor of the RNA helicase DHX9, exhibiting an IC50 of 4.3 nM. This compound is valuable for studies investigating the role of DHX9 in RNA processing and regulation, making it suitable for research applications in cancer biology and virology. Researchers can utilize DHX9-IN-5 to elucidate the molecular mechanisms underlying RNA helicase functions and their implications in disease.
WRN Inhibitor 4 is a selective inhibitor of the Werner Syndrome ATP-dependent helicase (WRN), demonstrating a pIC50 of ≥ 7. This compound effectively modulates WRN activity, making it a valuable tool for studying tumors characterized by a high mutation burden. Its application in cancer research aids in elucidating the role of WRN in genomic stability and tumorigenesis.
WRN Inhibitor 8 is a selective inhibitor of WRN helicase, exhibiting an IC50 value of 48 nM. This compound effectively impedes tumor cell proliferation and is valuable for research in cancer biology, particularly in studies focusing on mechanisms of tumor progression and the potential therapeutic avenues targeting WRN helicase.
NCGC00029283 is a potent inhibitor of Werner syndrome helicase-nuclease (WRN), exhibiting an IC50 of 2.3 μM for WRN helicase, along with IC50s of 12.5 μM and 3.4 μM for BLM and FANCJ helicases, respectively. This compound is valuable for studying the roles of helicases in DNA repair and replication pathways. It is particularly relevant for research on cellular mechanisms associated with Werner syndrome and various cancers linked to helicase dysfunction.
Werner syndrome RecQ helicase-IN-3 is a selective inhibitor of the Werner syndrome RecQ helicase (WRN), exhibiting an IC50 value of 0.06 µM. This compound demonstrates significant antiproliferative properties and has been investigated for its potential anticancer effects. It is a valuable tool for research focused on the molecular mechanisms underlying cancer and cellular aging associated with WRN dysfunction.
WRN Inhibitor 1 is an inhibitor of the Werner Syndrome helicase (WRN), targeting the helicase domain to impede its enzymatic activity. This compound is useful for investigating the role of WRN in cellular processes, particularly in cancer research, where its dysfunction contributes to genomic instability and tumor development. Researchers can employ WRN Inhibitor 1 to elucidate the molecular mechanisms associated with Werner Syndrome and related malignancies.
Werner syndrome RecQ helicase-IN-4 is a highly potent inhibitor of the Werner syndrome RecQ helicase (WRN), exhibiting an IC50 value of 0.06 µM. This compound demonstrates significant antiproliferative activity, making it a valuable tool for cancer research and therapeutic development. Its ability to inhibit WRN provides insights into the role of helicase activity in cellular processes and cancer progression.
MOMA-341 is a selective inhibitor of Werner RecQ-like helicase (WRN) that functions through an allosteric and ATP-competitive binding mechanism, targeting cysteine 727 of the enzyme. This compound exhibits significant antitumor activity, making it a valuable tool for research on advanced and metastatic solid tumors. Its ability to hinder WRN activity provides insights into cancer biology and the development of therapeutic strategies.
Werner syndrome RecQ helicase-IN-2 is a potent inhibitor of the Werner syndrome RecQ DNA helicase (WRN). Its primary mechanism of action involves the selective disruption of WRN activity, which plays a critical role in DNA repair and maintenance. This compound is valuable for cancer research, particularly in studies investigating the interplay between WRN function and tumorigenesis.
DHX9-IN-6 is an ATP-dependent inhibitor of RNA helicase A (DHX9), targeting its helicase activity. This compound exhibits significant potential for investigations in cancer research, particularly in studying the modulation of RNA metabolism and its implications in tumorigenesis. The selective inhibition of DHX9 could provide insights into therapeutic strategies for various cancers.
Synonyms: IDE275 (enantiomer)
GSK4418959 (enantiomer) is a selective, non-covalent WRN helicase inhibitor characterized by its reversible binding properties. It effectively inhibits ATPase activity and DNA unwinding in an ATP-competitive manner. This compound is particularly valuable for researching microsatellite instability-high (MSI-H) cancers, providing insights into therapeutic strategies targeting WRN helicase.
