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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DHX9-IN-12
0 ImagesCat. No.: HY-157609CAS No.: 2973747-13-4DHX9-IN-12 (83) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.917 μM in DHX9 cellular target engagement. Used in cancer research.
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WRN inhibitor 19
0 ImagesCat. No.: HY-176727WRN inhibitor 19 (Compound 40) is a WRN helicase inhibitor (IC50: 3.7 nM). WRN inhibitor 19 exhibits selective antiproliferative activity in WRN-dependent cancer cells. WRN inhibitor 19 inhibits WRN helicase function by competitively binding to the ATP site and induces DNA damage and cell cycle arrest. WRN inhibitor 19 can be used in the study of WRN-dependent cancers.
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WRN-IN-26
0 ImagesCat. No.: HY-183610CAS No.: 3059172-54-9WRN-IN-26 is an orally active Werner syndrome helicase (WRN) inhibitor with a human Ki value of 58.7 μM and an IC50 value of 0.026 μM. WRN-IN-26 selectively targets the cysteine residues of WRN. WRN-IN-26 induces the expression of p21 protein in MSI-H tumor cells. WRN-IN-26 inhibits the growth of MSI-H tumor cells and exhibits potent in vivo efficacy in MSI-H xenograft tumor models. WRN-IN-26 can be used for the research of microsatellite instability-high (MSI-H) cancers.
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(Rac)-Adibelivir hydrochloride
0 ImagesCat. No.: HY-150306CCAS No.: 2954725-84-7Synonyms: (Rac)-IM-250 hydrochloride(Rac)-Adibelivir hydrochloride ((Rac)-IM-250 hydrochloride) is a blood-brain barrier-penetrant HSV helicase-primase inhibitor and metabolic stabilizer with antiviral activity. (Rac)-Adibelivir hydrochloride is also effective against Acyclovir (HY-17422)-resistant strains, and its deuterated structure exhibits enhanced metabolic stability, reducing the formation of hydroxylated metabolites. (Rac)-Adibelivir prolongs in vivo half-life, reduces administration dosage, improves oral bioavailability, and achieves higher brain exposure in mice. (Rac)-Adibelivir hydrochloride can be used in the research of herpes simplex infection, herpes encephalitis and Alzheimer's disease.
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DHX9-IN-16
0 ImagesCat. No.: HY-157612CAS No.: 2973397-48-5DHX9-IN-16 (208) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.125 μM in DHX9 cellular target engagement. Used in cancer research.
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DHX9-IN-7
0 ImagesCat. No.: HY-157603CAS No.: 2973400-87-0DHX9-IN-7 (550) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.105 μM in DHX9 cellular target engagement. Used in cancer research.
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Methylbiocin
0 ImagesCat. No.: HY-162711CAS No.: 23370-12-9Methylbiocin is an ATP competitive inhibitor for human CMG helicase with an IC50 of 59 µM. Methylbiocin exhibits potential in cancer research.
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WRN inhibitor 10
0 ImagesCat. No.: HY-163797CAS No.: 3049092-06-7WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice.
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WRN-IN-22
0 ImagesCat. No.: HY-176912WRN-IN-22 (compound A01) is a potent Werner syndrome RecQ helicase (WRN) inhibitor (IC50 < 100 nM). WRN-IN-22 can be used for microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) cancer research, such as colorectal, gastric, prostate and endometrial cancer.
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WRN inhibitor 13
0 ImagesCat. No.: HY-164852CAS No.: 2923009-51-0WRN inhibitor 13 is a WRN helicase inhibitor with a pIC50 of 6-7.
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DHX9-IN-13
0 ImagesCat. No.: HY-157606CAS No.: 2973399-28-7DHX9-IN-13 (389) 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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WRN inhibitor 12
0 ImagesCat. No.: HY-168592CAS No.: 3044040-29-8WRN inhibitor 12 (compound 5) is an inhibitor of WRN helicase.
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Avenanthramide A-d4
0 ImagesCat. No.: HY-114977SAvenanthramide A-d4 is the deuterium labeled Avenanthramide A (HY-114977). Avenanthramide A is an orally active phytoalexin that targets the RNA helicase DDX3 with a KD of 8.8 μM. Avenanthramide A induces mitochondrial swelling and increased ROS production, and triggers apoptosis in CRC cells. Avenanthramide A inhibits smooth muscle cell proliferation and enhances nitric oxide production. Avenanthramide A can be used in research on colorectal cancer and atherosclerosis.
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Pritelivir-d4-1
0 ImagesCat. No.: HY-15303SSynonyms: AIC316-d4-1; BAY 57-1293-d4-1Pritelivir-d4-1 (AIC316-d4-1) is deuterium labeled Pritelivir. Pritelivir (AIC316), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir 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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WRN-IN-24
0 ImagesCat. No.: HY-181562CAS No.: 3113010-46-8WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer.
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Ledoxantrone trihydrochloride
0 ImagesCat. No.: HY-106305ACAS No.: 119221-49-7Synonyms: CI 958 trihydrochlorideLedoxantrone (CI 958) trihydrochloride is a DNA helicases inhibitor with an IC50 of 0.17 μM. Ledoxantrone trihydrochloride can be used in the study of prostate cancer.
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WRN inhibitor 7
0 ImagesCat. No.: HY-161386CAS No.: 444780-45-4WRN inhibitor 7 (Compound h6) is a WRN inhibitor. WRN inhibitor 7 effectively inhibits WRN's helicase and ATPase activity (IC50: 9.8 μM and 15.8 μM respectively). WRN inhibitor 7 can be used for research of microsatellite instable (MSI) cancers.
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TMV-IN-4
0 ImagesCat. No.: HY-152259CAS No.: 1820823-40-2
