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noncompetitive polymerase

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9

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137067
    IMT1B
    4 Publications Verification

    LDC203974

    		 DNA/RNA Synthesis Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects .
    IMT1B
  • HY-13859
    Clevudine

    L-FMAU

    		 HBV DNA/RNA Synthesis Orthopoxvirus Infection
    Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
    Clevudine
  • HY-154964
    RSV L-protein-IN-2

    		RSV Infection
    RSV L-protein-IN-2 (Compound A) is a noncompetitive RSV polymerase inhibitor (IC50: 4.5 μM). RSV L-protein-IN-2 shows antiviral activity against long RSV strains (EC50: 1.3 μM) .
    RSV L-protein-IN-2
  • HY-154967
    RSV L-protein-IN-4

    		RSV Infection
    RSV L-protein-IN-4 (Compound C) is a noncompetitive RSV polymerase inhibitor (IC50: 0.88 μM). RSV L-protein-IN-4 shows antiviral activity against RSV strains (EC50: 0.25 μM) .
    RSV L-protein-IN-4
  • HY-136650
    Fludarabine triphosphate

    F-ara-ATP

    		 Nucleoside Antimetabolite/Analog Drug Metabolite DNA/RNA Synthesis Apoptosis Cancer
    Fludarabine triphosphate (F-ara-ATP), the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis .
    Fludarabine triphosphate
  • HY-136650A
    Fludarabine triphosphate trisodium

    F-ara-ATP trisodium

    		 Nucleoside Antimetabolite/Analog Drug Metabolite DNA/RNA Synthesis Apoptosis Cancer
    Fludarabine triphosphate (F-ara-ATP) trisodium, the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate trisodium inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate trisodium inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis .
    Fludarabine triphosphate trisodium
  • HY-134539
    IMT1
    3 Publications Verification

    		 Oxidative Phosphorylation Mitochondrial Metabolism DNA/RNA Synthesis Metabolic Disease Cancer
    IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
    IMT1
  • HY-148396
    UCK2 Inhibitor-3

    		DNA/RNA Synthesis Infection Cancer
    UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM .
    UCK2 Inhibitor-3
  • HY-100513A
    Dehydroaltenusin

    		Apoptosis DNA/RNA Synthesis Antibiotic Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
    Dehydroaltenusin

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