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 (161)
Related Products (161)
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Fluoroneplanocin A-8N
0 ImagesCat. No.: HY-179249Fluoroneplanocin A-8N (Compound 3a) is an inhibitor targeting SAH hydrolase (IC50 = 1.51 μM) and viral RNA polymerase. Fluoroneplanocin A-8N exhibits broad-spectrum anti-SARS-CoV-2 and dengue virus activity, with EC50 values of 12.2 and 37.4 μM respectively. Fluoroneplanocin A-8N has no cytotoxicity. Fluoroneplanocin A-8N can be used for anti-positive-strand viruses.
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DENV-IN-4
0 ImagesCat. No.: HY-115929CAS No.: 2762302-75-8DENV-IN-4 is a potent DENV inhibitor (DENV EC50=4.79 μM, Vero CC50>100 μM, SI>20.9). DENV-IN-4 can inhibit the expression level of DENV2 with concentration-dependence and reduce RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 has antiviral effect.
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RNAP-σ interaction inhibitor-1
0 ImagesCat. No.: HY-171647CAS No.: 2408055-45-6RNAP-σ interaction inhibitor1 (compound 5d) is an inhibitor of RNA polymerase-sigma factors interaction. RNAP-σ interaction inhibitor-1 exhibits the activity against Streptococci with MIC values of 1-2 µg/mL.
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Simeprevir-13C,d3
0 ImagesCat. No.: HY-10241SSynonyms: TMC435-13C,d3; TMC435350-13C,d3Simeprevir-13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir 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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PAN endonuclease-IN-1
0 ImagesCat. No.: HY-163147CAS No.: 2378640-67-4PAN endonuclease-IN-1 (Compound 23) is a potent PAN endonuclease inhibitor, with Kd values of 277 μM, 384 μM and 328 μM for WT, I38T and E23K PAN endonucleases, respectively. The RNA-dependent RNA polymerase acidic N-terminal (PAN) endonuclease, a critical component of influenza viral replication machinery, is an antiviral target.
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CYP2C19-IN-1
0 ImagesCat. No.: HY-151254CAS No.: 3010895-53-8CYP2C19-IN-1 (compound 20d) is a potent CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C19-IN-1 inhibits RNA-dependent RNA polymerase (RdRP) with a Ki value of 6.16 µM. CYP2C19-IN-1 can be used in study of anti-ZIKV.
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Favipiravir sodium
0 ImagesCat. No.: HY-14768ACAS No.: 1366418-99-6Synonyms: T-705 sodiumFavipiravir (T-705) sodium is an inhibitor of viral RNA polymerase (RNA polymerase), which is converted into its active form Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the activity of influenza virus RNA-dependent RNA polymerase (RdRP) with an IC50 of 341 nM.
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POLRMT-IN-3
0 ImagesCat. No.: HY-181071POLRMT-IN-3 is a photosensitive inhibitor of mitochondrial RNA polymerase (POLRMT). POLRMT-IN-3 is biologically inactive in the dark but rapidly releases the active parent compound LJ03 upon illumination with 405 nm light, enabling spatiotemporally precise inhibition of POLRMT. POLRMT-IN-3 exhibits antitumor activity and can be used in research on tumors such as pancreatic cancer and ovarian cancer.
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Cap-dependent endonuclease-IN-2
0 ImagesCat. No.: HY-143743CAS No.: 2303917-78-2Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28).
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2'-Deoxy-2'-fluoro-l-uridine
0 ImagesCat. No.: HY-148167CAS No.: 622785-69-72'-Deoxy-2'-fluoro-l-uridine is an L-nucleoside compound. 2'-Deoxy-2'-fluoro-l-uridine is a potent, selective viral RNA polymerase inhibitor, thereby inhibiting RNA virus replication.
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POLRMT-IN-4
0 ImagesCat. No.: HY-181072CAS No.: 3121040-39-6POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer.
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ε-Amanitin
0 ImagesCat. No.: HY-131083CAS No.: 21705-02-2ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II.
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Triptolide-6-succinate-β-D-glucose
0 ImagesCat. No.: HY-177903CAS No.: 2003231-25-0Triptolide-6-succinate-β-D-glucose (Compound 2) is a glucose-conjugated derivative of Triptolide (HY-32735). Triptolide-6-succinate-β-D-glucose is a tumor-selective prodrug targeting glucose transporters ( GLUT). Triptolide-6-succinate-β-D-glucose can induce the degradation of the RPB subunit of RNA polymerase II. Triptolide-6-succinate-β-D-glucose inhibits the proliferation of HEK293T cells with an IC50 value of 268 nM. Triptolide-6-succinate-β-D-glucose can be used for the research of cancer, such as prostatic cancer.
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RdRP-IN-4
0 ImagesCat. No.: HY-144668CAS No.: 3035088-22-0RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice.
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YH-0623
0 ImagesCat. No.: HY-175454YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research.
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RdRP-IN-10
0 ImagesCat. No.: HY-181778CAS No.: 3099256-57-9RdRP-IN-10 is a SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor with an IC50 value of 5.78 μM. RdRP-IN-10 forms covalent binds with SARS-CoV-2 nsp8 Cys114, disrupts nsp8-nsp12 stabilizing interactions. RdRP-IN-10 inhibits SARS-CoV-2 RdRp-mediated RNA polymerization without interfering with RNA-RdRp complex binding. RdRP-IN-10 exerts antiviral effects in cellular models. RdRP-IN-10 can be used for the research of SARS-CoV-2 infection.
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2'-(2-Nitrobenzyl)-ATP trisodium
0 ImagesCat. No.: HY-171632A2'-(2-Nitrobenzyl)-ATP trisodium is a rATP analog. 2'-(2-Nitrobenzyl)-ATP trisodium acts as a transcription terminator, inhibiting further RNA chain elongation by T7 RNA polymerase.
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RNAP-σ interaction inhibitor-2
0 ImagesCat. No.: HY-171648CAS No.: 3077454-53-3RNAP-σ interaction inhibitor-2 (compound 7d) is an inhibitor of RNA polymerase-sigma factors interaction. RNAP-σ interaction inhibitor-2 exhibits the activity against S. aureus with MIC values of 2 µg/mL.
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Beclabuvir hydrochloride
0 ImagesCat. No.: HY-12429ACAS No.: 958002-36-3Synonyms: BMS-791325 hydrochlorideBeclabuvir (BMS-791325) hydrochloride is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
