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 (158)
Related Products (158)
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Metalaxyl-M
0 ImagesSynonyms: (R)-MetalaxylMetalaxyl-M ((R)-Metalaxyl) is an orally active and selective inhibitor of fungal RNA polymerase, which exerts fungicidal activity by selectively interfering with the synthesis of fungal ribosomal RNA. Metalaxyl-M can also be used to induce inflammation in hepatocytes and regulate tryptophan metabolism. Metalaxyl-M can be used in ecotoxicology studies.
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Galidesivir hydrochloride
0 ImagesSynonyms: BCX4430 hydrochloride; Immucillin-A hydrochlorideGalidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride 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 hydrochloride inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
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Filibuvir
0 ImagesFilibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation.
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MC-VC-PABC-C6-α-Amanitin
0 ImagesMC-VC-PABC-C6-α-Amanitin is a Drug-Linker Conjugates for ADC, consisting of an anticancer toxin alpha-Amanitin (HY-19610) and a MC-VC-PABC-C6 linker. Among them, alpha-Amanitin is a potent inhibitor of RNA polymerase IIα.
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Oncrasin-1
0 ImagesOncrasin-1 is an RNA polymerase inhibitor. Oncrasin-1 suppresses the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells. Oncrasin-1 effectively kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 leads to coaggregation of PKCι and splicing factors into megaspliceosomes. Oncrasin-1 induces malfunction in the RNA processing machinery. Oncrasin-1 is an anti-cancer agent and can therefore be studied in research for lung cancer.
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BPR3P0128
0 ImagesBPR3P0128 is an orally active, non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that has been shown to inhibit the activity of various SARS-CoV-2 variants. The EC50 for SARS-CoV-2 and HCoV-229E are 0.62 μM and 0.14 μM. BPR3P0128 demonstrates effective anti-pancoronavirus activity within the submicromolar range. PR3P0128 shows synergistic antiviral activity when combined with Remdesivir (HY-104077).
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POL1-IN-1
0 ImagesPOL1-IN-1 is a class of RNA polymerase I inhibitors with broad-spectrum antiproliferative activity against tumor cells, while selectively inhibiting RNA polymerase I transcription. By blocking RNA polymerase I-mediated rRNA synthesis, POL1-IN-1 impairs ribosome biogenesis, thereby inhibiting tumor cell proliferation and inducing apoptosis. POL1-IN-1 can be used for the research of malignant tumors.
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MMV688845
0 ImagesSynonyms: (R)-GSK1729177AMMV688845 is a nontuberculous mycobacteria (NTM) RNA polymerase inhibitor with bactericidal activity against Mycobacterium abscessus and anti-tuberculosis efficacy.
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MTR-106
0 ImagesMTR-106 is a potent and orally active G-quadruplex stabilizer and RNA polymerase I inhibitor. MTR-106 induces apoptosis and inhibits cell growth. MTR-106 can be used in research of cancer.
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Pseudouridimycin
0 ImagesCat. No.: HY-125650CAS No.: 1566586-52-4Synonyms: PUMPseudouridimycin (PUM) is an antibiotic that selectively inhibits bacterial RNA polymerase (RNAP), with an IC50 of about 0.1 μM and MICs of 4-6 μg/mL. Pseudouridimycin is a C-nucleoside analogue that's effective against both Gram-negative and Gram-positive bacteria. Pseudouridimycin inhibits bacterial growth in vitro and shows activity in a mouse model of purulent streptococcal peritonitis.
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7-Aminoactinomycin D (solution)
0 Images7-Aminoactinomycin D (solution) (7-AAD (solution)) 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.
Solvent and concentration: DMSO: 1 mg/mL
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3'-Deoxyuridine-5'-triphosphate trisodium solution (100 mM)
0 ImagesCat. No.: HY-135780APurity: 99.66%Synonyms: 3'-dUTP trisodium3'-Deoxyuridine-5'-triphosphate trisodium (3'-dUTP trisodium) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate trisodium strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM.
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DNA31
0 ImagesCat. No.: HY-128917CAS No.: 845626-57-5DNA31 is a potent RNA polymerase inhibitor.
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BMH-22
0 ImagesBMH-22, a benzonaphthyridin, is a RNA polymerase I (Pol I) transcription inhibitor independent of p53 function. BMH-22 causes reorganization of nucleolar marker proteins consistent with segregation of the nucleolus. BMH-22 destabilizes RPA194 in a proteasome-dependent manner and inhibits nascent rRNA synthesis and expression of the 45S rRNA precursor. BMH-22 shows potent anticancer activity across many tumor types.
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RdRP-IN-2
0 ImagesRdRP-IN-2 is a RNA dependent RNA polymerase (RdRp) inhibitor. RdRP-IN-2 significantly inhibits SARS-CoV-2 RdRp with an IC50 of 41.2 μM.RdRP-IN-2 also inhibits Feline coronavirus (FIPV) replication.
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Pipobroman
0 ImagesPipobroman is a bromide derivative of piperazine and acts as an alkylating agent. Pipobroman plays its role by inhibiting DNA and RNA polymerase or by reducing pyrimidine nucleotide incorporation into DNA. Pipobroman can be used for the cancer research, including polycythemia vera, myeloproliferative neoplasm, and AML et.al.
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Anti-Influenza agent 10
0 ImagesCat. No.: HY-180269Anti-Influenza agent 10 (Compound 41) is an influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor. Anti-Influenza agent 10 exhibits potent antiviral activity against A/PR/8/34(H1N1) with an IC50 of 0.29μM and a KD of 4.11 μM. Anti-Influenza agent 10 can inhibit the assembly of the viral RdRp complex by disrupting the protein interaction between PA and PB1 subunits, thereby blocking the transcription and replication of the viral genome. Anti-Influenza agent 10 shows significant broad-spectrum effects on multiple influenza virus strains, such as H3N2, H3N8 and H9N2 with IC50 values of 3.96, 1.91 and 1.45 μM. Anti-Influenza agent 10 can be used for the research of influenza A Virus Infection.
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2,5-Di-tert-butyl-1,4-benzoquinone
0 Images2,5-Di-tert-butyl-1,4-benzoquinone is a potent antibacterial agent that defends the emerging antibacterial resistance, which is found in marine Streptomyces sp. VITVSK1. 2,5-Di-tert-butyl-1,4-benzoquinone is also a potent inhibitor of RNA polymerase.
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Fidaxomicin-d7
0 ImagesCat. No.: HY-17580SCAS No.: 2143934-06-7Fidaxomicin-d7 (OPT-80-D7) is the deuterium labeled Fidaxomicin. Fidaxomicin (OPT-80), a macrocyclic RNA polymerase inhibitor, has a narrow spectrum of activity. Fidaxomicin selectively eradicates pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora.
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3'-Deoxyuridine-5'-triphosphate
0 ImagesCat. No.: HY-135780CAS No.: 69199-40-2Synonyms: 3'-dUTP3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM.
