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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Thiolutin
0 ImagesThiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC)[1][2][3][4][5].
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Onradivir
0 ImagesSynonyms: ZSP1273Onradivir (ZSP1273) is an orally active antiviral agent targeting influenza A virus RNA polymerase PB2 subunit with an IC50 of 0.562 nM. Onradivir inhibits cap binding to influenza A virus RNA polymerase PB2 subunit, suppresses viral replication, reduces viral titres and RNA loads, and inhibits influenza A virus infection. Onradivir maintains high survival rates in influenza A virus-infected mice, and reduces influenza A virus titers in a murine model. Onradivir can be used for the research of influenza A virus infection.
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β-Amanitin
0 ImagesCat. No.: HY-125586CAS No.: 21150-22-1β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
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iPAF1C
0 ImagesiPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4+T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders).
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JNJ-8003
0 ImagesJNJ-8003 is a potent and orally active non-nucleoside RSV polymerase inhibitor with an IC50 of 0.29 nM. JNJ-8003 targets the L protein polymerase complex of RSV (IC50 = 0.67 nM), and blocks the transcription and replication of the viral genome by inhibiting the activity of RNA-dependent RNA polymerase (RdRp). JNJ-8003 displays subnanomolar activity in vitro as well as prominent efficacy in mice and a neonatal lamb models. JNJ-8003 can be used for the study of respiratory syncytial virus (RSV).
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(±)-Enitociclib
0 ImagesSynonyms: (±)-BAY-1251152; (±)-VIP152(±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.
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Metarrestin
0 ImagesSynonyms: ML246Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
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Ethynylcytidine
0 ImagesSynonyms: ECyD; TAS-106; 3'-C-EthynylcytidineEthynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis, inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer. Ethynylcytidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Beclabuvir
0 ImagesSynonyms: BMS-791325Beclabuvir 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.
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γ-Amanitin
0 ImagesCat. No.: HY-131081CAS No.: 21150-23-2γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin. γ-Amanitin competitively binds to monoclonal antibody (mAb), with an IC50 of 163.1 ng/mL. γ-Amanitin is toxic to a variety of cells.
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Rifalazil
0 ImagesSynonyms: KRM-1648; ABI-1648Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB).
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Balapiravir
0 ImagesCat. No.: HY-10443CAS No.: 690270-29-2Synonyms: Ro 4588161; R1626Balapiravir (Ro 4588161; R1626) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity. Balapiravir is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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AVG-233
0 ImagesAVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC50=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV).
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LL-K12-18
0 ImagesLL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer.
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T7 RNA polymerase
0 ImagesT7 RNA polymerase is a polymerase expressed by Escherichia coli from the RNA polymerase gene of T7 bacteriophage. T7 RNA polymerase is highly specific and involved in in vitro transcription (IVT) of mRNA. In the presence of Mg2+, T7 RNA polymerase only uses the single-stranded or double-stranded DNA containing the T7 promoter sequence as a template, and uses NTP as a substrate to synthesize RNA complementary to the single-stranded DNA downstream of the promoter.
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R-1479
0 ImagesSynonyms: 4'-AzidocytidineR-1479 (4'-Azidocytidine), a nucleoside analogue, is a specific inhibitor of RNA-dependent RNA polymerase (RdRp) of HCV. R-1479 inhibits HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM). R-1479 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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KI-DX-014
0 ImagesKI-DX-014 is a DDX21 inhibitor with high RNA-binding inhibitory activity (IC50 of 3.31 μM). KI-DX-014 targets DDX21’s intrinsically disordered C-terminal domain, inhibits DDX21-structured RNA interaction, modulates DDX21’s RNA-dependent ATPase activity, and disrupts DDX21 biomolecular condensate formation. KI-DX-014 attenuates in vitro P-TEFb release from the 7SK snRNP complex, suppresses P-TEFb-dependent RNA polymerase II CTD phosphorylation, and induces developmental defects in zebrafish embryos. KI-DX-014 acts as a chemical probe for dissecting DDX21 functions in normal physiology and disease states. KI-DX-014 can be used for cancers and neurodegenerative disorders research.
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HeE1-2Tyr
0 ImagesCat. No.: HY-100749CAS No.: 2245195-67-7HeE1-2Tyr, a pyridobenzothiazole compound, is a flavivirus RNA dependent RNA polymerases (RdRp) inhibitor. HeE1-2Tyr significantly inhibits West Nile, Dengue and SARS-CoV-2 RdRps (IC50 of 27.6 μM) activity in vitro.
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AS-136A
0 ImagesAS-136A is an orally active non-nucleoside inhibitor of the measles virus RNA-dependent RNA polymerase (RdRp) with an IC50 of 2 µM for measles virus.
