RNA Polymerases
RNA polymerases catalyze genome transcription, converting genetic information into RNA outputs that support gene expression, ribosome biogenesis, protein synthesis, and cell growth[1]. In eukaryotic cells, three nuclear enzymes divide this work: RNA polymerase I (Pol I) transcribes ribosomal DNA, RNA polymerase II (Pol II) produces mRNAs and many regulatory non-coding RNAs, and RNA polymerase III (Pol III) generates tRNAs, 5S rRNA, and other short non-coding RNAs[2][3]. Mechanistically, Pol I and Pol III support ribosome production and translation capacity, whereas Pol II links transcription initiation, elongation, RNA processing, and gene-specific regulation through its C-terminal domain[4]. In disease models, disruption of Pol I or Pol III function produces tissue-specific developmental disorders, especially craniofacial abnormalities and leukodystrophy or neurodegenerative phenotypes[3]. Compared with Pol II, Pol I and Pol III are distinguished by high-output non-coding RNA transcription and by specialized subunits that define isoform-specific transcription programs[2][3]. For experimental applications, Pol I inhibition with CX-5461 suppresses rDNA transcription and has been used to study p53 activation, nucleolar stress, DNA damage response, and cancer cell vulnerability[5][6]. Pol III inhibition also provides aging-model utility, because reduced Pol III activity extends lifespan in yeast, worms, and flies downstream of TORC1[7].
References:
- [1]. Barba-Aliaga M, et al. Eukaryotic RNA Polymerases: The Many Ways to Transcribe a Gene. Front Mol Biosci. 2021 Apr 21;8:663209. [Content Brief]
- [2]. Wang Y, et al. BMP and RA signaling cooperate to regulate Apolipoprotein C1 expression during embryonic development. Gene. 2015 Jan 10;554(2):196-204. [Content Brief]
- [3]. Watt KE, et al. RNA Polymerases I and III in development and disease. Semin Cell Dev Biol. 2023 Feb 28;136:49-63. [Content Brief]
- [4]. Hsin JP, et al. The RNA polymerase II CTD coordinates transcription and RNA processing. Genes Dev. 2012 Oct 1;26(19):2119-37. [Content Brief]
- [5]. Bywater MJ, et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer Cell. 2012 Jul 10;22(1):51-65. [Content Brief]
- [6]. Haddach M, et al. Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics. ACS Med Chem Lett. 2012 May 8;3(7):602-6. [Content Brief]
- [7]. Filer D, et al. RNA polymerase III limits longevity downstream of TORC1. Nature. 2017 Dec 14;552(7684):263-267. [Content Brief]
All Product Categories
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RNA Polymerases Related Products (165)
Related Products (165)
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CX-5461
0 ImagesCX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors.
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Favipiravir
0 ImagesSynonyms: T-705Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
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Guanosine triphosphate disodium
0 ImagesSynonyms: GTP disodiumGuanosine triphosphate (GTP) disodium is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate disodium promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate disodium links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate disodium accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate disodium is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
The product specifications provided below refer solely to the active content of Guanosine triphosphate disodium.
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IMT1
0 ImagesIMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases.
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Dihydromyricetin
0 ImagesSynonyms: Ampelopsin; AmpeloptinDihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
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Guanosine triphosphate trisodium
0 ImagesCat. No.: HY-12695CAS No.: 36051-31-7Synonyms: GTP trisodiumGuanosine triphosphate (GTP) trisodium is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate trisodium promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate trisodium links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate trisodium accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate trisodium is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
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BMH-21
0 ImagesBMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity.
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IMT1B
0 ImagesSynonyms: LDC203974IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
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Simeprevir
0 ImagesSynonyms: TMC435; TMC435350Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
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Cynaroside
0 ImagesSynonyms: Luteolin 7-glucoside; Luteolin 7-O-β-D-glucosideCynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM. Cynaroside also is a promising inhibitor for H2O2-induced apoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities.
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CX-5461 dihydrochloride
0 ImagesCat. No.: HY-13323APurity: 99.41%CX-5461 dihydrochloride is a selective, orally active RNA polymerase I inhibitor. CX-5461 dihydrochloride disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 dihydrochloride upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 dihydrochloride induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 dihydrochloride can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors.
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Enitociclib
0 ImagesSynonyms: (+)-BAY-1251152; (+)-VIP152; (S)-EnitociclibEnitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC50=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma.
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7-Aminoactinomycin D
0 Images7-Aminoactinomycin D (7-AAD) a cell-impermeant fluorescent DNA stain, is a potent RNA polymerase inhibitor. 7-Aminoactinomycin D selectively binds to GC regions of the DNA. 7-Aminoactinomycin D also has antibacterial effects.
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Fidaxomicin
0 ImagesSynonyms: OPT-80; PAR-101Fidaxomicin (OPT-80), a macrocyclic antibiotic, is an orally active and potent RNA polymerase inhibitor. Fidaxomicin has a narrow spectrum of antibacterial activity and a good anti-Clostridium difficile activity (MIC90=0.12 μg/mL). Fidaxomicin can be used for Clostridium difficile infection (CDI) research.
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Rifabutin
0 ImagesSynonyms: Ansamycin; LM-427Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.
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Rifaximin
0 ImagesRifaximin, a gastrointestinal-selective antibiotic, binds the β-subunit of bacterial DNA-dependent RNA polymerase, resulting in inhibition of bacterial RNA synthesis. Rifaximin susceptibility is higher against Gram-positive strains (MIC: 0.03-5 mg/ml) compared to Gram-negative bacteria (MIC: 8-50 mg/mL).
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Dirhodium tetraacetate
0 ImagesSynonyms: Tetrakis(acetato)dirhodium(II); Rhodium(II) acetate dimerDirhodium tetraacetate (Tetrakis (acetato) dirhodium (II)) is an anticancer agent. Dirhodium tetraacetate functionally inhibits the activities of DNA polymerase I and RNA polymerase. It also acts as a catalyst and can be used to construct rhodium-based artificial metalloenzymes.
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Guanosine triphosphate trisodium salt hydrate
0 ImagesCat. No.: HY-12695BCAS No.: 207300-85-4Synonyms: GTP trisodium salt hydrateGuanosine triphosphate (GTP) trisodium salt hydrate is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate trisodium salt hydrate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate trisodium salt hydrate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate trisodium salt hydrate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate trisodium salt hydrate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
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Galidesivir
0 ImagesSynonyms: BCX4430; Immucillin-AGalidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
