helicase

Werner syndrome RecQ helicase-IN-1 is a potent Werne r syndrome RecQ DNA deconjugase (WRN) inhibitor that can be used to study cancers such as colon and stomach cancer.

Werner syndrome RecQ helicase-IN-4 is an effective inhibitor of Werner syndrome RecQ DNA helicase (WRN), exhibiting anticancer and antiproliferative activities, used for colorectal and gastric cancer research.

Werner syndrome RecQ helicase-IN-3, a potent and orally active inhibitor of Werner syndrome RecQ helicase (WRN), exhibits anticancer and antiproliferative activities with an IC50 value of 0.06 µM.

Werner syndrome RecQ helicase-IN-2 is an effective inhibitor of Werner syndrome RecQ DNA helicase (WRN), used in studying colorectal and gastric cancer.

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).

GSK4418959 (IDE275) is an orally active, non-covalent, reversible, and selective WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used to study MSI-H related research.

ML328 is a potent and selective inhibitor of bacterial AddAB(IC50 = 1.0 μM) and RecBCD(IC50 = 4.8 μM) helicase-nucleases.

NCGC00029283 is a potent inhibitor of Werner syndrome helicase-nuclease (WRN), displaying inhibitory activity against WRN helicase with an IC 50 value of 2.3 μM. Additionally, it exhibits inhibitory effects on Bloom syndrome protein helicase (BLM) and Fanconi anemia group J protein helicase (FANCJ) with IC 50 values of 12.5 μM and 3.4 μM, respectively.

Brr2-IN-3 (Brr2 Inhibitor C9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa (a group of progressive retinal degenerative disorders).

N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)pyrazine-2-carboxamide exhibit an inhibitory effect on bacterial DNA helicases, nucleases, or helicase-nuclease enzyme complexes, such as, for example, one or more enzymes selected from the RecBCD and AddAB families of enzymes.

Eubananin effectively inhibits the ATPase activity of the SARS Coronavirus helicase, displaying an IC50 value of 2.8 μM.

Iodobananin effectively inhibits the ATPase activity of the SARS Coronavirus helicase, displaying an IC 50 value of 0.54 μM.

BPK-21 is an active acrylamide compound that effectively suppresses T cell activation by blocking the function of ERCC3, a helicase enzyme. BPK-21 specifically targets C342 within the ERCC3 helicase.

Pritelivir mesylate is active against herpes simplex virus types 1 and 2 (IC50: 0.02 μM against HSV1-2). Pritelivir mesylate is an inhibitor of the viral helicase-primase complex. Pritelivir mesylate shows antiviral activity in vitro and in animal models

Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand that inhibits FANCJ and DinG helicases with IC50s of 65±6 nM and 50±10 nM, respectively.

GSK_WRN4 is a WRN helicase inhibitor with anticancer activity. It induces DNA double-strand breaks and inhibits MSI tumor cell growth, making it useful in cancer research.

WRN inhibitor 7 (Compound h6), a potent inhibitor of Werner syndrome helicase, demonstrates effective suppression of WRN's helicase and ATPase activities with IC50 values of 9.8 μM and 15.8 μM, respectively. This compound is utilized in the study of microsatellite instable (MSI) cancers [1].

GBM CSCs-IN-1 (Compound (−)-20), a rocaglate derivative, potently inhibits glioblastoma stem cells (GBM CSCs) and exhibits an EC50 of 45 nM by targeting the RNA helicase DDX3. Additionally, it induces apoptosis in these cells.

DHX9-IN-8 (Compound 6) functions as an inhibitor of the RNA helicase DHX9, exhibiting an EC50 of 3.4 μM for cellular target engagement within DHX9. It is primarily utilized in cancer research [1].

DHX9-IN-9 (509) acts as an inhibitor of the RNA helicase DHX9, demonstrating an EC50 of 0.0177 μM in DHX9 cellular target engagement, primarily utilized in cancer research [1].

CMLD012073 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits NIH 3T3 cells (IC50: 10 nM). CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).

WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN). This inhibitor is applicable in cancer research [1].

SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective small-molecule inhibitor of nsp13 helicase, inhibiting the ssDNA+ ATPase activity of nsp13 with an IC50 of 57 μM, and providing a broad-spectrum antiviral effect.

FWM-3, a potent SARS-CoV-2 NSP13 helicase inhibitor, has demonstrated efficacy [1].