DNA Polymerases
DNA polymerases maintain genome integrity by synthesizing DNA during replication, repair, recombination, translesion synthesis, and checkpoint-associated processes[1]. In eukaryotic DNA replication, Pol α initiates synthesis with RNA/DNA primers, while Pol δ and Pol ε extend DNA from primer ends[2]. Mechanistically, evidence supports Pol ε as the primary leading-strand replicase and Pol δ as the main lagging-strand replicase at the eukaryotic replication fork[3]. In DNA repair, base excision repair (BER) corrects oxidative, deamination, and alkylation damage, then uses polymerase-dependent repair synthesis and ligation to restore DNA continuity[4]. Compared with replicative isoforms, Pol β functions as a BER enzyme whose polymerase and dRP lyase activities coordinate gap filling and sugar-phosphate removal[5]. In mitochondria, Pol γ differs from nuclear polymerases because it is the only known human mitochondrial DNA polymerase and is essential for mitochondrial DNA replication and repair[6]. In damage-tolerance models, Pol η differs from high-fidelity replicative polymerases by enabling bypass of UV-induced thymine dimers, and POLH defects define xeroderma pigmentosum variant cells[7]. For experimental applications, aphidicolin inhibits B-family DNA polymerases and provides a tool for probing replication-dependent DNA synthesis[8].
References:
- [1]. Hubscher U, et al. Eukaryotic DNA polymerases. Annu Rev Biochem. 2002;71:133-63. [Content Brief]
- [2]. Chilkova O, et al. The eukaryotic leading and lagging strand DNA polymerases are loaded onto primer-ends via separate mechanisms but have comparable processivity in the presence of PCNA. Nucleic Acids Res. 2007;35(19):6588-97. [Content Brief]
- [3]. Miyabe I, et al. The major roles of DNA polymerases epsilon and delta at the eukaryotic replication fork are evolutionarily conserved. PLoS Genet. 2011 Dec;7(12):e1002407. [Content Brief]
- [4]. Krokan HE, et al. Base excision repair. Cold Spring Harb Perspect Biol. 2013 Apr 1;5(4):a012583. [Content Brief]
- [5]. Kumar A, et al. Interlocking activities of DNA polymerase β in the base excision repair pathway. Proc Natl Acad Sci U S A. 2022 Mar 8;119(10):e2118940119. [Content Brief]
- [6]. Vanselow C, et al. Genetic analysis of the Photosystem I subunits from the red alga, Galdieria sulphuraria. Biochim Biophys Acta. 2009 Jan;1787(1):46-59. [Content Brief]
- [7]. Masutani C, et al. The XPV (xeroderma pigmentosum variant) gene encodes human DNA polymerase eta. Nature. 1999 Jun 17;399(6737):700-4. [Content Brief]
- [8]. Baranovskiy AG, et al. Structural basis for inhibition of DNA replication by aphidicolin. Nucleic Acids Res. 2014 Dec 16;42(22):14013-21. [Content Brief]
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DNA Polymerases Related Products (158)
Related Products (158)
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1,4-Naphthoquinone-d6
0 Images1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone. 1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models.
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Polθ-IN-8
0 ImagesPolθ-IN-8 (example 77) is a DNA polymerase theta (Polθ) inhibitor with an c of <100 nM for Polθ ATPase activity. Polθ-IN-8 can be used to study diseases related to Polθ activity (such as cancer).
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2'-Deoxyadenosine-5'-triphosphate-d14 (dilithium)
0 ImagesCat. No.: HY-136648S3CAS No.: 2687960-68-3Synonyms: dATP-d14 dilithium2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
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AZT triphosphate
0 ImagesCat. No.: HY-116364CAS No.: 92586-35-1Synonyms: 3'-Azido-3'-deoxythymidine-5'-triphosphateAZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
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AZT triphosphate TEA
0 ImagesCat. No.: HY-116364ASynonyms: 3'-Azido-3'-deoxythymidine-5'-triphosphate TEAAZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) TEA is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TEA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TEA also inhibits the DNA polymerase of HBV. AZT triphosphate TEA activates the mitochondria-mediated apoptosis pathway.
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Apricitabine
0 ImagesSynonyms: SPD754; AVX754Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection.
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Fiacitabine
0 ImagesSynonyms: NSC 382097; FIAC; FOACFiacitabine (NSC 382097; FIAC; FOAC) is a potent and highly selective anti-herpesvirus agent. Fiacitabine acts as an inhibitor of HSV DNA polymerase, with a Ki of 0.26 μM for HSV-1 and 0.42 μM for HSV-2, respectively. Fiacitabine can be efficiently phosphorylated by thymidine kinase encoded by the virus itself to generate FIACTP, an active triphosphate metabolite. Fiacitabine is applicable to research related to herpesvirus infections.
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Ganciclovir triphosphate
0 ImagesCat. No.: HY-131605CAS No.: 86761-38-8Synonyms: GCV-TPGanciclovir triphosphate (GCV-TP) is a competitive DNA polymerase inhibitor and a metabolite of Ganciclovir (HY-13637). Ganciclovir triphosphate can replace Guanine-5'-triphosphate to terminate DNA chain extension, and mimics dGTP (HY-138616) to compete with mammalian DNA polymerases. Ganciclovir triphosphate can be used in research related to HSV infection, retinoblastoma, glioblastoma and colorectal cancer.
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Cytarabine-d2
0 ImagesCytarabine-d2 is the deuterium labeled Cytarabine. Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV.
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Roseoside
0 ImagesCat. No.: HY-N1341CAS No.: 54835-70-0Roseoside is an inhibitor of DNA gyrase and HAV 3C protease, and also inhibits HCV NS5A/B replicase in human systems with an IC50 of 20 μM. Roseoside binds to the active site of enzymes and stabilizes the interaction by forming hydrogen bonds with key amino acid residues. Roseoside inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, and Candida albicans, and interferes with HCV RNA replication in vitro by inhibiting HCV NS5A/B replicase (IC50=20 μM). Roseoside shows no cytotoxicity and serves as a research tool for studies related to bacterial infections, candidiasis, HAV and HCV.
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DNA polymerase-IN-6
0 ImagesCat. No.: HY-170547CAS No.: 2701561-91-1DNA polymerase-IN-6 is an antiviral agent and a DNA polymerase inhibitor. DNA polymerase-IN-6 inhibits the replication of HCMV, HSV-1, HSV-2 and EBV. DNA polymerase-IN-6 exhibits low cytotoxicity in mammalian cells. DNA polymerase-IN-6 can be used in research related to viral infections.
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3'-Fluorothymidine-5'-triphosphate tetrasodium
0 ImagesSynonyms: 3'-FdTTP tetrasodium3'-Fluorothymidine-5'-triphosphate tetrasodium (3'-FdTTP tetrasodium) is a dTTP (HY-138615) analog. 3'-Fluorothymidine-5'-triphosphate tetrasodium inhibits the T4 DNA polymerases competitively with dTTP. 3'-Fluorothymidine-5'-triphosphate tetrasodium inhibits DNA synthesis by T4 wild-type, L98 and CB121 DNA polymerase.
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Fludarabine triphosphate
0 ImagesCat. No.: HY-136650CAS No.: 74832-57-8Synonyms: F-ara-ATPFludarabine 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.
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FF-10502
0 ImagesCat. No.: HY-115528CAS No.: 184302-49-6FF-10502, a structural analog of Gemcitabine, is a pyrimidine nucleoside antimetabolite. FF-10502 inhibits DNA polymerase α and β. FF-10502 shows beneficial anticancer activity via a mechanism of action on dormant cells.
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RTx-303
0 ImagesCat. No.: HY-179219SCAS No.: 3035072-99-9RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer.
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Cidofovir dihydrate
0 ImagesSynonyms: GS 0504 dihydrate; HPMPC dihydrate; (S)-HPMPC dihydrateCidofovir (GS 0504; HPMPC; (S)-HPMPC) dihydrate is an acyclic monophosphate nucleotide analogue and CMV inhibitor with antiviral activity. Cidofovir dihydrate inhibits cytomegalovirus (CMV) replication by selectively inhibiting viral DNA polymerase. Cidofovir dihydrate induces apoptosis and can be used in studies of AIDS cytomegalovirus retinitis, herpes, and cancer. Cidofovir dihydrate also has anti-orthopoxvirus and anti-variola activities.
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AZD4956
0 ImagesCat. No.: HY-183630CAS No.: 3045469-78-8AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors.
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Cidofovir diphosphate
0 ImagesCat. No.: HY-131606CAS No.: 142276-31-1Cidofovir diphosphate is an active intracellular metabolite of Cidofovir. Cidofovir diphosphate is a selective inhibitor of viral DNA polymerases with Ki values of 6.6, 0.86 and 1.4 μM for HCMV, HSV-1 and HSV-2 DNA polymerase, respectively.
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(+)-Plakevulin A
0 ImagesCat. No.: HY-N13095CAS No.: 518035-27-3(+)-Plakevulin A (Plakevulin A) is an oxylipin and can be isolated from an Okinawan sponge Plakortis sp. (+)-Plakevulin A inhibits the enzymatic activity of DNA polymerases α and δ. (+)-Plakevulin A induces apoptosis and shows anticancer activity.
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Polθ-IN-5
0 ImagesCat. No.: HY-169284CAS No.: 3058636-12-4Polθ-IN-5 (Compound 139) is a DNA polymerase theta (Polθ) inhibitor. Polθ-IN-5 has antitumor activity.
