RNA Polymerases Inhibitor

MMV688845 is a nontuberculous mycobacteria (NTM) RNA polymerase inhibitor with bactericidal activity against Mycobacterium abscessus and anti-tuberculosis efficacy.

MTR-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.

Pseudouridimycin (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.

7-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

3'-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 K_i value of 2.0 μM.

DNA31 is a potent RNA polymerase inhibitor.

BMH-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.

Pipobroman 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.

Anti-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 K_D 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.

2,5-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.

3'-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 K_i value of 2.0 μM.

Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a K_i of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC₅₀ of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (M^pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.

Guanosine triphosphate-¹³C₁₀,¹⁵N₅ tetraammonium solution (100 mM) (GTP-¹³C₁₀,¹⁵N₅ tetraammonium) is the ¹⁵N, ¹³C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate 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 accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.

Metalaxyl-M-d₆ ((R)-Metalaxyl-d₆) is the deuterium labeled Metalaxyl-M (HY-B0843A). Metalaxyl-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.

GS-441524 hydrochloride is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 hydrochloride competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 hydrochloride inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 hydrochloride reduces viral RNA levels in cats. GS-441524 hydrochloride can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19).

Guanosine triphosphate-d₁₄ dilithium (GTP-d₁₄ dilithium) is the deuterated-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate 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 accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.

Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity. Balapiravir (hydrochloride) 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.

Dasabuvir (ABT-333) sodium is a nonnucleoside hepatitis C virus (HCV) polymerase inhibitor. Dasabuvir sodium inhibits RNA-dependent RNA polymerase encoded by the HCV NS5B gene. Dasabuvir sodium inhibits genotype 1a (strain H77) and 1b (strain Con1) replicons, with EC₅₀ values of 7.7 and 1.8 nM, respectively.

Onradivir (ZSP1273) monohydrate is an orally active antiviral agent targeting influenza A virus RNA polymerase PB2 subunit with an IC₅₀ of 0.562 nM. Onradivir monohydrate 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 monohydrate maintains high survival rates in influenza A virus-infected mice, and reduces influenza A virus titers in a murine model. Onradivir monohydrate can be used for the research of influenza A virus infection.

Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I K_i: 40.9 μM; RNA polymerase II K_i: 38.0 μM).