RNA Polymerases Inhibitor

GS-646089 is a broad-spectrum antiviral nucleoside analog that exhibits significant inhibitory activity against respiratory syncytial virus (RSV), human metapneumovirus (hMPV), rhinovirus (enterovirus) and enteroviruses. The IC₅₀ of GS-646089 targeting RNA-dependent RNA polymerase (RdRp) ranges from 43 to 46 nM. GS-646089 blocks viral replication by being converted into a triphosphate metabolite intracellularly, which competes with ATP for incorporation into nascent RNA strands and acts as an immediate chain terminator. GS-646089 is the parent compound of the double prodrug GS-7682 (HY-161877), and is used in studies of acute respiratory viral infections and infections caused by related pathogens.

RNA polymerase-IN-4 is a RNA polymerase inhibitor with an EC₅₀ of 22.81 nM. RNA polymerase-IN-4 exhibits potent anti-influenza virus activity (EC₅₀ = 3.76 nM), relatively low cytotoxicity (CC₅₀ = 29.91 μM). RNA polymerase-IN-4 can be used for the research of infection, such as influenza virus infection.

RNA polymerase-IN-1 (compound 4) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-1 inhibits CYP isozymes.

Rifamycin AF-013 is a derivative of Rifamycin (HY-B1907). Rifamycin AF-013 inhibits DNA polymerase γ by competing with dTTP and template primers for binding. Rifamycin AF-013 exhibits inhibitory activity against Rifampicin (HY-B0272)-resistant RNA polymerase. Rifamycin AF-013 inhibits non-polymerase enzymes including glutamic-oxaloacetic transaminase (GOT), glutamic-pyruvic transaminase (GPT), and Alkaline phosphatase. Rifamycin AF-013 can be used in research related to Rifampicin-resistant bacterial infections and Ehrlich ascites tumors.

RNA polymerase-IN-2 (compound 5) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-2 inhibits CYP isozymes.

KJ001-12a is an orally active anti-influenza agent with activity against influenza A and B strains. KJ001-12a acts as an RNA-dependent RNA polymerase inhibitor that reduces the expression levels of viral M2 mRNA and vRNA. KJ001-12a shows low sensitivity to the loss of inhibitory activity caused by the I38T mutation. KJ001-12a is applicable for influenza-related research.

Pseudouridimycin (PUM) TFA 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 TFA is a C-nucleoside analogue that's effective against both Gram-negative and Gram-positive bacteria. Pseudouridimycin TFA inhibits bacterial growth in vitro and shows activity in a mouse model of purulent streptococcal peritonitis.

Favipiravir-¹³C3 is the ¹³C labeled isotope of Favipiravir (HY-14768). Favipiravir (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.

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

HCV-IN-50 (Compound 2) is a competitive and selective HCV NS5B RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 0.3  μM for NS5B △C21 enzyme over △C55 enzyme. HCV-IN-50 has an antiviral activity and efficiently blocks replication of HCV subgenomic replicons especially mutant replicons.

2'-(2-Nitrobenzyl)-ATP is an rATP analog. 2'-(2-Nitrobenzyl)-ATP acts as a transcription terminator, inhibiting further RNA chain elongation by T7 RNA polymerase.

(E)-Antiviral agent 67 (compound PC6) is a pyrazolone-based antiviral agent with certain inhibitory activity against RNA-dependent RNA polymerase.

CX-5461 (Standard) is the analytical standard of CX-5461 (HY-13323). This product is intended for research and analytical applications. CX-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.

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.

MRL-436 is a RNA polymerase inhibitor with antibacterial activity. MRL-436 exerts its antibacterial activity dependent on residue 622 of the RNA polymerase β' subunit and the RNAP ω subunit. MRL-436 inhibits Rifampicin (HY-B0272)-resistant RNA polymerase derivatives and exhibits antibacterial activity against Rifampicin-resistant strains.