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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DNA polymerase
0 ImagesDNA polymerase is a polymerase agent targeting DNA templates. DNA polymerase catalyzes the polymerization of deoxyribonucleotides (dNTPs) to extend DNA strands with high fidelity and processivity. DNA polymerase is promising for research of cancers.
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Morindone
0 ImagesMorindone is an anthraquinone found in Morinda citrifolia L. Morindone can inhibit cancer cells proliferation, induce apoptosis and cause G1 phase arrest. Morindone can inhibit activities of DNA polymerase and downregulate mutated TP53 and KRAS gene expression. Morindone can be used for the research of cancer, such as colon cancer.
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Eprociclovir
0 ImagesCat. No.: HY-16740CAS No.: 145512-85-2Synonyms: A-5021Eprociclovir is an antiviral drug with nucleoside analogues. The triphosphate form of Eprociclovir 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 is against herpes viruses, including but not limited to cytomegalovirus (CMV) and herpes simplex virus (HSV). Eprociclovir can be used in studies interfered with by sensitive viruses.
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Petasiphenol
0 ImagesCat. No.: HY-N21777CAS No.: 145904-50-3Petasiphenol is a phenolic natural product found in Petasites japonicus, possessing selective inhibitory activity against DNA polymerase λ. Petasiphenol binds to the N-terminal BRCT domain of DNA polymerase λ, with an IC50 of 7.8 μM against DNA polymerase λ. Petasiphenol induces cell growth inhibition, G1 phase cell cycle arrest in human cancer cell lines, and exhibits anti-inflammatory activity against TPA-induced mouse ear inflammation. Petasiphenol can be used for research on cancer and inflammation-related diseases.
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Acyclovir monophosphate
0 ImagesCat. No.: HY-17422BCAS No.: 66341-16-0Acyclovir monophosphate is a potent anti-herpes simplex virus (HSV) agent. Acyclovir monophosphate blocks DNA synthesis through the inhibition of the viral DNA polymerase and terminates the chain elongation of the viral DNA. Acyclovir monophosphate shows antitumor activity.
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Resveratrol (GMP)
0 ImagesResveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
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Multi-target kinase-IN-9
0 ImagesCat. No.: HY-182037Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research.
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2'-Deoxyadenosine-5'-triphosphate-15N5 (dilithium)
0 ImagesCat. No.: HY-136648S4Purity: 99.30%Synonyms: dATP-15N5 dilithium2'-Deoxyadenosine-5'-triphosphate-15N5 (dATP-15N5) dilithium is 15N 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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Polθ-IN-6
0 ImagesCat. No.: HY-169285CAS No.: 3058496-94-6Polθ-IN-6 (Compound 89) is a DNA polymerase theta (Polθ) inhibitor. Polθ-IN-6 has antitumor activity.
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4-Demethoxy-7,9-di-epi-daunorubicin
0 ImagesCat. No.: HY-160968CAS No.: 58957-91-84-Demethoxy-7,9-di-epi-daunorubicin, a derivative of Daunorubicin (HY-13062A), is an anthracycline antibiotics. 4-Demethoxy-7,9-di-epi-daunorubicin can bind to calf thymus DNA and forms a complex with the stacked DNA base pairs. 4-Demethoxy-7,9-di-epi-daunorubicin can inhibit prokaryotic nucleic acid polymerases, including E. coli DNA polymerase I and RNA polymerase. 4-Demethoxy-7,9-di-epi-daunorubicin can be used for researches of cancer and infection.
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Cidofovir diphosphate-13C3
0 ImagesCat. No.: HY-131606SCidofovir diphosphate-13C3 is the 13C-labeled Cidofovir diphosphate (HY-131606). Cidofovir diphosphate is the intracellular active metabolite of Cidofovir (HY-17438) and its oral prodrug Brincidofovir (HY-14532). By inhibiting viral DNA polymerase (Ki ≈ 76.3 μM), cidofovir diphosphate is widely used in studies on double-stranded DNA virus infections, including cytomegalovirus (CMV), adenovirus (AdV), and poxviruses (such as monkeypox and molluscum contagiosum virus, MCV).
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Procyanidin B3-3-O-gallate
0 ImagesCat. No.: HY-N16549CAS No.: 86631-41-6Synonyms: 3-O-Galloylprocyanidin B3Procyanidin B3-3-O-gallate (3-O-Galloylprocyanidin B3) is a selective mammalian DNA polymerase α inhibitor, with a calf DNA polymerase α IC50 of 0.26 μM. Procyanidin B3-3-O-gallate scavenges DPPH radicals. Procyanidin B3-3-O-gallate can be used for research on oxidative stress and inflammatory diseases[1].
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DNA polymerase-IN-7
0 ImagesCat. No.: HY-178063DNA polymerase-IN-7 is a noncompetitive inhibition of DNA Polymerase β with an IC50 of 112 nM and a Ki of 35 nM. DNA polymerase-IN-7 can inhibit DNA pol β lyase activity and the binding of the lyase domain of Pol β to DNA. DNA polymerase-IN-7 can be used for the research of cancer, such as cervical cancer.
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Polθ-IN-9
0 ImagesCat. No.: HY-179413CAS No.: 3050552-13-8Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC50 = 9.6 nM, Kd = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib (HY-10162), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer.
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Cidofovir sodium
0 ImagesCat. No.: HY-167911CAS No.: 127749-27-3Synonyms: GS 0504 sodium; HPMPC sodium; (S)-HPMPC sodiumCidofovir sodium is an acyclic monophosphate nucleotide analogue and CMV inhibitor with antiviral activity. Cidofovir sodium inhibits cytomegalovirus (CMV) replication by selectively inhibiting viral DNA polymerase. Cidofovir sodium induces apoptosis and can be used in studies of AIDS cytomegalovirus retinitis, herpes, and cancer. Cidofovir sodium also has anti-orthopoxvirus and anti-variola activities.
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IAG-10
0 ImagesIAG-10 is a selective DNA polymerase kappa (hpol κ) inhibitor with an IC50 value of 7.2 μM. IAG-10 exerts its function by disrupting the formation of the binary complex between the enzyme and DNA. IAG-10 enhances the antiproliferative and DNA-damaging activities of Temozolomide (HY-17364) in tumor cells with functional hpol κ expression. IAG-10 can be used in the research of cancers such as malignant brain tumors.
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HIV-1 inhibitor-42
0 ImagesCat. No.: HY-147903CAS No.: 2459929-46-3HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM.
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Polθ-IN-11
0 ImagesCat. No.: HY-183748CAS No.: 3082173-75-6Polθ-IN-11 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. Polθ-IN-11 activates the cGAS-STING pathway. Polθ-IN-11 upregulates the expression of PD-L1 in HR-deficient cancer cells. Polθ-IN-11 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. Polθ-IN-11 can be used in studies related to HR-deficient cancers.
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BVDU 5′-Triphosphate
0 ImagesCat. No.: HY-W747737CAS No.: 77222-61-8Synonyms: (E)-5-(2-Bromovinyl)-dUTP; BVdUTPBVDU 5′-Triphosphate is an antivirus agent with 5′-Triphosphate label, targeting viral DNA polymerase. BVDU 5′-Triphosphate shows excellent selectivity against varicella-zoster virus (VZV) and herpes simplex virus type 1 (HSV-1), due to a specific phosphorylation by the virus-encoded thymidine kinase.
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DNA polymerase-IN-3
0 ImagesCat. No.: HY-155094CAS No.: 381689-75-4DNA polymerase-IN-3 (Compd 5b) is a coumarin derivative that exhibits inhibitory activity against Taq DNA polymerase and can be used in proliferative disease research.
