Helicases
Helicases are ATP-driven nucleic acid motor enzymes that translocate along DNA or RNA, unwind duplex substrates, and disrupt protein-nucleic acid interactions[1]. Mechanistically, helicases support DNA replication, repair, recombination, transcription, ribosome biogenesis, RNA splicing, RNA transport, RNA editing, and RNA degradation[1][2]. In disease-relevant models, human RECQ helicases maintain genome stability, and loss of BLM, WRN, or RECQL4 function causes Bloom syndrome, Werner syndrome, and Rothmund-Thomson-related syndromes[3]. Compared with RECQ DNA helicases, DDX3X is an X-linked DEAD-box RNA helicase with a Y-linked paralog, DDX3Y, and DDX3X-linked conditions can show sex differences related to paralog expression or function[4]. For experimental applications, ML216 inhibits BLM DNA unwinding activity and modulates chromosome stability in human cells[5]. DDX3X inhibitors have been designed, validated on the target enzyme, and evaluated against West Nile virus infection, supporting helicase inhibition as a tool for antiviral research[6]. RK-33 has also been used to target DDX3X in breast cancer bone metastasis models[7].
References:
- [1]. Abdelhaleem M. Helicases: an overview. Methods Mol Biol. 2010;587:1-12. [Content Brief]
- [2]. Umate P, et al. Genome-wide comprehensive analysis of human helicases. Commun Integr Biol. 2011 Jan;4(1):118-37. [Content Brief]
- [3]. Monnat RJ Jr. Human RECQ helicases: roles in DNA metabolism, et al. Human RECQ helicases: roles in DNA metabolism, mutagenesis and cancer biology. Semin Cancer Biol. 2010 Oct;20(5):329-39. [Content Brief]
- [4]. Gadek M, et al. The variant landscape and function of DDX3X in cancer and neurodevelopmental disorders. Trends Mol Med. 2023 Sep;29(9):726-739. [Content Brief]
- [5]. Nguyen GH, et al. A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells. Chem Biol. 2013 Jan 24;20(1):55-62. [Content Brief]
- [6]. Brai A, et al. DDX3X Helicase Inhibitors as a New Strategy To Fight the West Nile Virus Infection. J Med Chem. 2019 Mar 14;62(5):2333-2347. [Content Brief]
- [7]. Winnard PT Jr, et al. Targeting RNA helicase DDX3X with a small molecule inhibitor for breast cancer bone metastasis treatment. Cancer Lett. 2024 Nov 1;604:217260. [Content Brief]
All Product Categories
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Helicases Related Products (107)
Related Products (107)
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ZL-12A probe
0 ImagesZL-12A probe is a "stereoprobe "that can promote the degradation of TFIIH helicase ERCC3. ZL-12A degrades ERCC3 by covalently modifying C342.
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WRN inhibitor 2
0 ImagesWRN inhibitor 2 (example 118) is a WRN (Werner Syndrome ATP dependent helicase enzyme) inhibitor, with pIC50 ≥ 7.0.
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MOMA-341
0 ImagesCat. No.: HY-175750CAS No.: 3078276-74-8MOMA-341 is a selective Werner RecQ like helicase (WRN) inhibitor. MOMA-341 binds to WRN at cysteine 727 through an allosteric and ATP-competitive binding mechanism. MOMA-341 has antitumor activity and can be used for advanced and metastatic solid tumors research.
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Pritelivir mesylate hydrate
0 ImagesSynonyms: AIC316 mesylate hydrate; BAY 57-1293 mesylate hydratePritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2.
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GSK4418959 (enantiomer)
0 ImagesCat. No.: HY-169422ACAS No.: 3064599-37-4Synonyms: IDE275 (enantiomer)GSK4418959 enantiomer is an enantiomer of GSK4418959 (HY-169422). GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. 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.
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TK216-d4
0 ImagesTK216-d4 is the deuterium labeled TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
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WRN inhibitor 11
0 ImagesCat. No.: HY-168583CAS No.: 3058317-61-3WRN inhibitor 11 (Example 17) is an orally active inhibitor of WRN helicase, with the IC50 of 63 nM.
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GBM CSCs-IN-1
0 ImagesCat. No.: HY-161946CAS No.: 3080542-96-4GBM CSCs-IN-1 (Compound (−)-20), a derivative of rocaglate, is a potent inhibitor of glioblastoma stem cells (GBM CSCs) with an EC50 of 45 nM, functioning by targeting the RNA helicase DDX3. Furthermore, GBM CSCs-IN-1 is also capable of inducing apoptosis.
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WRN inhibitor 17
0 ImagesCat. No.: HY-169423CAS No.: 3064599-40-9WRN inhibitor 17 (Compound 250) is an orally active Werner Syndrome ATP dependent helicase enzyme (WRN) inhibitor, in particular inhibit WRN helicase domain activity. WRN inhibitor 17 is promising for research of cancers.
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DHX9-IN-8
0 ImagesCat. No.: HY-157602CAS No.: 2973746-64-2DHX9-IN-8 (Compound 6) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research.
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SARS-CoV-2 nsp13-IN-4
0 ImagesCat. No.: HY-150625CAS No.: 923140-39-0SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective nsp13 helicase small-molecule inhibitor and inhibit the ssDNA+ ATPase activity of nsp13 with an IC50 value of 57 μM. SARS-CoV-2 nsp13-IN-4 is agentlike molecule with molecular weight of less than 450Da and can provide a broad-spectrum antiviral effect.
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DHX9-IN-14
0 ImagesCat. No.: HY-157610CAS No.: 2973747-90-7DHX9-IN-14 (161) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research.
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DHX9-IN-15
0 ImagesCat. No.: HY-157607CAS No.: 2973398-27-3DHX9-IN-15 (287) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.232 μM in DHX9 cellular target engagement. Used in cancer research.
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RecQ helicase-IN-1
0 ImagesCat. No.: HY-161151Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor. Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells.
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Ledoxantrone
0 ImagesCat. No.: HY-106305CAS No.: 113457-05-9Synonyms: CI 958Ledoxantrone (CI 958) is a DNA helicases inhibitor with an IC50 of 0.17 μM. Ledoxantrone can be used in the study of prostate cancer.
