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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Telomeric G4s ligand 2
0 ImagesCat. No.: HY-181850CAS No.: 3094716-52-3Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC50 of 0.4 μM. Telomeric G4s ligand 2 binds to dimeric telomeric G4, inhibits the activities of DHX36 and BLM helicases. Telomeric G4s ligand 2 activates cGAS-STING and TERRA-ZBP1 pathways, inducing autophagy and G2/M cell cycle arrest, and exhibits antiproliferative effects across cancer cell lines. Telomeric G4s ligand 2 can be used for the study of colorectal cancer.
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WRN-IN-19
0 ImagesCat. No.: HY-174217CAS No.: 3058652-58-4WRN-IN-19 (Compound (S)-27) is a covalent WRN helicase inhibitor, with pIC50 (0 h/4 h) = 5.4/7.5 in the DNA-unwinding 5 endpoint assays. WRN-IN-19 shows synthetic lethality in MSI-H (high microsatellite instability) cancer cells.
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FWM-3
0 ImagesCat. No.: HY-146987CAS No.: 714923-33-8FWM-3 is a potent SARS-CoV-2 NSP13 helicase inhibitor.
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Fli-1-IN-1
0 ImagesCat. No.: HY-163325ACAS No.: 3027140-81-1Fli-1-IN-1 (compound 21) is a FLI1 targeting agent that directly binds to and inhibits the EWS-FLI1 protein interaction. EWS-FLI1 can bind to RNA helicase A, and Fli-1-IN-1 inhibits EWS-FLI1 and has potential anticancer activity.
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DHX9-IN-11
0 ImagesCat. No.: HY-157605CAS No.: 2973402-91-2DHX9-IN-11 (469) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.0838 μM in DHX9 cellular target engagement. Used in cancer research.
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DHX9-IN-10
0 ImagesCat. No.: HY-157608CAS No.: 2973746-79-9DHX9-IN-10 (49) is a RNA helicase DHX9 inhibitor, with an EC50 of 9.04 μM in DHX9 cellular target engagement. Used in cancer research.
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Fli-1-IN-1 fumarate
0 ImagesCat. No.: HY-163325Fli-1-IN-1 (compound 21) fumarate is a FLI1 targeting agent that directly binds to and inhibits the EWS-FLI1 protein interaction. EWS-FLI1 can bind to RNA helicase A, and Fli-1-IN-1 fumarate inhibits EWS-FLI1 and has potential anticancer activity.
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DHX9-IN-17
0 ImagesCat. No.: HY-157611CAS No.: 2973397-26-9DHX9-IN-17 (186) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.161 μM in DHX9 cellular target engagement. Used in cancer research.
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SARS-CoV-2-IN-19
0 ImagesCat. No.: HY-146379CAS No.: 2244991-17-9SARS-CoV-2-IN-19 (Compound 6g) is a potent inhibitor of SARS-CoV-2 with an EC50 of 8.8 μM. SARS-CoV-2-IN-19 shows potent activity against SARS-CoV-2 helicase (nsp13), a highly conserved enzyme, highlighting a potentiality against emerging HCoVs outbreaks. SARS-CoV-2-IN-19 has the potential for the research of infection diseases.
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DHX9-IN-18
0 ImagesCat. No.: HY-160813CAS No.: 2973395-40-1DHX9-IN-13 (Example 1) is a RNA helicase DHX9 inhibitor with an EC50 of 16.4 μM. DHX9-IN-13 exhibits biochemical infection point of 0.32 μM. DHX9-IN-13 can be used for the study of cancers.
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WRN-IN-23
0 ImagesCat. No.: HY-179326CAS No.: 2923008-65-3WRN-IN-23 is a Werner Syndrome helicase enzyme (WRN) inhibitor. WRN-IN-23 inhibits the ATP-dependent helicase domain activity of WRN. WRN-IN-23 can be used for the research of cancers characterized by microsatellite instability (MSI) and/or defective DNA mismatch repair system (dMMR).
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Cyclothialidine B
0 ImagesCat. No.: HY-N14130CAS No.: 194276-76-1Cyclothialidine B inhibits escherichia coli DNA helicases with an IC50 of 0.7 μM.
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Cyclothialidine D
0 ImagesCat. No.: HY-N14131CAS No.: 194276-78-3Cyclothialidine D inhibits escherichia coli DNA helicases with an IC50 of 0.7 μM.
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(Rac)-Adibelivir
0 ImagesCat. No.: HY-150306ACAS No.: 2137928-83-5Synonyms: (Rac)-IM-250(Rac)-Adibelivir ((Rac)-IM-250) is a blood-brain barrier-penetrant HSV helicase-primase inhibitor and metabolic stabilizer with antiviral activity. (Rac)-Adibelivir 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 can be used in the research of herpes simplex infection, herpes encephalitis and Alzheimer's disease.
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Heliquinomycin
0 ImagesCat. No.: HY-105387CAS No.: 178182-49-5Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth.
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Cyclothialidine E
0 ImagesCat. No.: HY-N14132CAS No.: 194276-79-4Cyclothialidine E inhibits escherichia coli DNA helicases with an IC50 of 0.7 μM.
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SGC-NSP2hel-1
0 ImagesCat. No.: HY-176268Synonyms: RA-0188293; RA-NSP2-1SGC-NSP2hel-1 (RA-0188293), a chemical probe, is a potent, specific and orally active nsP2 inhibitor. SGC-NSP2hel-1 has broad spectrum activity against multiple alphaviruses of the nsP2 helicase with a CC50 > 250 μM. SGC-NSP2hel-1 (RA-0188293) shows selectivity index > 4000 against human RNA helicases. SGC-NSP2hel-1 reduces virus replication and limited virus-induced pathology by forming a stable complex with nsP2 and ATP in a preclinical small animal model of CHIKV disease.
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CHIKV nsP2 protease-IN-2
0 ImagesCat. No.: HY-175234CAS No.: 3107145-13-8CHIKV nsP2 protease-IN-2 (Compound 2o) is a allosteric nonstructural protein 2 helicase (nsP2hel) inhibitor with IC50s of 0.5 μM and 0.9 μM for nsP2 ATPase and RNA unwindase, respectively. CHIKV nsP2 protease-IN-2 has broad-spectrum antialphaviral activity against chikungunya virus (CHIKV), Mayaro virus (MAYV), and Venezuelan equine encephalitis virus (VEEV) (EC50 of 120 nM for CHIKV-nLuc). CHIKV nsP2 protease-IN-2 can be used for alphaviruses infections research.
