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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RECQL5-IN-1
0 ImagesRECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells.
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GSK_WRN4
0 ImagesGSK_WRN4 is an orally active WRN helicase inhibitor (pIC50=7.6). GSK_WRN4 induces DNA damage markers (p21, p-γH2AX, p-KAP1). GSK_WRN4 selectively inhibits microsatellite-unstable tumor growth in vitro and in vivo by inducing DNA double-strand breaks, particularly at expanded TA repeats and regions of DNA damage.
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BPK-21
0 ImagesBPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3.
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DHX9-IN-5
0 ImagesDHX9-IN-5 (compound 277) is a RNA helicase DHX9 inhibitor with an IC50 of 4.3 nM.
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Sennidin B
0 ImagesSennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
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WRN inhibitor 5
0 ImagesWRN inhibitor 5, a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 5 can be used for the research of cancer, including cancers characterized by microsatellite instability (MSI) and/or defective DNA mismatch repair system (dMMR).
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Werner syndrome RecQ helicase-IN-3
0 ImagesWerner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity.
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Adibelivir
0 ImagesSynonyms: IM-250
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Brr2-IN-3
0 ImagesBrr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC50 value of 1.3 μM.
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Werner syndrome RecQ helicase-IN-4
0 ImagesWerner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity.
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NCGC00029283
0 ImagesNCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC50s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively.
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Pritelivir mesylate
0 ImagesSynonyms: AIC316 mesylate; BAY 57-1293 mesylatePritelivir mesylate (BAY 57-1293 mesylate), 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 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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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.
