DNA Polymerases Inhibitor

Dehydroeburiconic acid is a DNA polymerase α/β inhibitor, with IC₅₀ values of 40.8 μM and 30.0 μM against calf DNA polymerase α and rat DNA polymerase β, respectively. Dehydroeburiconic acid can be used in studies related to lanostane-type triterpenoids and DNA polymerase.

NSC-124854 is a DNA polymerase β (Pol-β) inhibitor with an IC₅₀ of 5.3 μM. NSC-124854 has antitumor activity.

Phosphonoacetic acid Standard is the analytical standard of Phosphonoacetic acid (HY-128744). This product is intended for research and analytical applications. Phosphonoacetic acid is a potent antiviral agent. Phosphonoacetic acid inhibits a variety of herpesviruses, orthopoxviruses, and retroviruses. Phosphonoacetic acid strongly inhibits viral and cellular DNA polymerase, reverse transcriptase, and terminal deoxynucleotidyl transferase activities in a non-competitive or uncompetitive manner by binding to the pyrophosphate site of the enzyme. Phosphonoacetic acid is useful for research related to lymphoid leukemia, herpesvirus infection, and vaccinia virus skin lesions.

Eprociclovir potassium is an antiviral drug with nucleoside analogues. The triphosphate form of Eprociclovir potassium is converted into the active form within virus-infected cells by the virus and possible cellular enzymes, including the viral thymidine kinase, thereby inhibiting the activity of the viral DNA polymerase. The primary activity of Eprociclovir potassium is against herpes viruses, including but not limited to cytomegalovirus (CMV) and herpes simplex virus (HSV). Eprociclovir potassium can be used in studies interfered with by sensitive viruses.

Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas.

ddATP (2',3'-Dideoxyadenosine 5'-triphosphate) tetrasodium is an active metabolite of 2',3'-dideoxyadenosine and an inhibitor of chain elongation by DNA polymerase (DNA polymerase). ddATP tetrasodium can be used in Sanger sequencing and research related to viral infections.

ddATP (2',3'-Dideoxyadenosine 5'-triphosphate), an active metabolite of 2',3'-dideoxyinosine, is a chain-elongating inhibitor of DNA polymerase. ddATP can be used for Sanger method for DNA sequencing and research of virus infection.

Valomaciclovir is a DNA polymerase inhibitor, potentially used for the treatment of acute herpes zoster and Epstein-Barr virus infection.

Cytarabine 5′-monophosphate is a metabolite of the nucleoside analog Cytarabine (HY-13605), catalyzed by deoxycytidine kinase. Cytarabine 5′-monophosphate is incorporated into DNA by DNA polymerase α, which reduces the rate of DNA synthesis. At a concentration of 15 mM, Cytarabine 5′-monophosphate inhibits nuclear and mitochondrial DNA replication in Saccharomyces cerevisiae (S. cerevisiae). Additionally, Cytarabine 5′-monophosphate (3.5-75.1 mg/kg) improves survival in leukemia mice (L1210 mice). Cytarabine 5′-monophosphate can be used in cancer research.

Eprociclovir sodium is an antiviral drug with nucleoside analogues. The triphosphate form of Eprociclovir sodium is converted into the active form within virus-infected cells by the virus and possible cellular enzymes, including the viral thymidine kinase, thereby inhibiting the activity of the viral DNA polymerase. The primary activity of Eprociclovir sodium is against herpes viruses, including but not limited to cytomegalovirus (CMV) and herpes simplex virus (HSV). Eprociclovir sodium can be used in studies interfered with by sensitive viruses.

α-Rubromycin (Collinomycin) is an antibiotic isolated from the mycelia of Streptomyces collinus. α-Rubromycin also acts as a DNA polymerase inhibitor, with an IC₅₀ of 0.91 μM against bovine mammalian DNA polymerase. α-Rubromycin binds to the active region of DNA polymerase β, competes with nucleotide substrates for binding, and interferes with template-DNA interactions. α-Rubromycin inhibits the activities of telomerase, retroviral reverse transcriptase and terminal deoxynucleotidyl transferase, as well as the growth of Staphylococcus aureus. α-Rubromycin can be used in studies related to bacterial infections.

Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a K_i of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer.

DNA polymerase-IN-2 (Compd 3c), a coumarin derivative, exhibits inhibitory activity against Taq DNA polymerase with IC₅₀ of 48.25 μM , which can be used in value-added disease research.

S-Chromene is a selective DNA polymerase-β (DNA pol-β) inhibitor. S-Chromene exhibits strong electrostatic complementarity with DNA pol-β but weak interaction with primase p58.

DNA polymerase-IN-1 (compound 2d) is a DNA polymerase inhibitor (IC₅₀=20.7 μM) with antiproliferative activity against tumor cells.

HO 221 is an orally active benzoylphenylurea derivative with antitumor activity. HO 221 can inhibit the activity of mammalian DNA polymerase alpha. HO 221 can induce G1 phase arrest. HO 221 can be used for the research of cancer, such as leukemia.

Procaspase-IN-5 is a human DNA polymerase λ inhibitor. Procaspase-IN-5 has DNA polymerization function and TdT function with an IC₅₀ value of 5.9 μM and 4.5 μM, respectively. Procaspase-IN-5 can be used for the research of cancer.

PMEG-DP disodium is a potent DNA polymerase inhibitor (IC₅₀=2.5 μM), especially for DNA polymerase α and δ. PMEG-DP disodium acts as an active metabolite of G-9191, which effectively inhibits the growth of papillomavirus (HPV) -infected cell lines. PMEG-DP disodium can be used in the study of HPV-related diseases.

Aphidicolin 17-acetate is a selective eukaryotic DNA polymerase α inhibitor. Aphidicolin 17-acetate does not inhibit DNA polymerase β and γ. Aphidicolin 17-acetate markedly inhibits the in vivo DNA synthesis of sea urchin embryos and HeLa cells but not RNA and protein syntheses.

Miboplatin (DWA-2114R), a platinum compound, is a DNA synthesis inhibitor. Miboplatin reduces its template activity for prokaryotic and eukaryotic DNA polymerases.