dna polymerase δ

Fludarabine Phosphate (NSC 312887 Phosphate) is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.

T2AA (4-[4-[(2S)-2-amino-3-hydroxypropyl]-2,6-diiodophenoxy]phenol) is an inhibitor of proliferating cell nuclear antigen (PCNA) with IC50 of 1 μM for PCNA/PIP-box peptide interaction. T2AA suppresses cancer cell growth and causes DNA replication stress by stalling DNA replication forks and inhibiting PCNA interaction with DNA polymerase δ.

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

DNA polymerase-IN-1, a DNA polymerase inhibitor, exhibited antiproliferative activity against tumor cells with a half-inhibitory concentration (IC50) of 20.7 μM. DNA polymerase-IN-1 inhibited Taq DNA polymerase with an IC50 of less than 250 μM. DNA polymerase-IN-1 was shown to inhibit Taq DNA polymerase by RT- DNA polymerase-IN-1 showed antiretroviral activity in vitro by RT-PCR assay and can be used to study oxidative damage and colorectal cancer.

Idoxuridine (Dendrid) is an analog of DEOXYURIDINE that inhibits viral DNA synthesis. The drug is used as an antiviral agent.

Ergocalciferol (Vitamin D2 (Calciferol)) is a derivative of ergosterol formed by ultraviolet rays breaking of the C9-C10 bond with a strong inhibitory effect against bladder tumor promotion by sodium saccharin, and it induces cell differentiation in leukemia cells. Vitamin D2 is an inhibitor of DNA Polymerase.

Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an acyclovir prodrug that, upon metabolism, inhibits viral DNA replication.

Cytarabine hydrochloride (Ara-C hydrochloride) is a nucleoside analog that causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC 50 of 16 nM. Cytarabine hydrochloride has antiviral effects against HSV.

Vidarabine (Adenine Arabinoside) is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.

Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) is a highly soluble cholesterol analogue often used in polar solutions for its hepatoprotective, anticancer and tumour growth inhibiting properties. Cholesteryl Hemisuccinate inhibits the hepatotoxicity of acetaminophen and prevents AAP-induced apoptosis and necrosis in hepatocytes. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase, thereby inhibiting DNA replication and repair as well as cell division.

3,4-Dihydroxybenzylamine hydrobromide (NSC-263475 hydrobromide) inhibits DNA polymerase activity in melanoma cells and displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.

Famciclovir (BRL 42810) is a Herpes Simplex Virus Nucleoside Analog DNA Polymerase Inhibitor. The mechanism of action of famciclovir is as a DNA Polymerase Inhibitor, and DNA Polymerase Inhibitor.

Isoindigotin is used in the therapy of Y.

RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Polθ), manifests remarkable oral activity. With an IC 50 value of 5.8 nM in the PicoGreen assay, RP-6685 effectively hinders the enzymatic activity of Polθ. In addition, it demonstrates significant antitumor efficacy as observed in a mouse tumor xenograft model [1].

Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine has a long half-life and shows significant reduction of covalently closed circular DNA (cccDNA), therefore the patient is less likely to have a relapse after treatment is discontinued.

1. Neobavaisoflavone is isolated as a DNA polymerase inhibitor. 2. Neobavaisoflavone might be a potential anabolic agent to treat bone loss-associated diseases. 3. Neobavaisoflavone has anti-inflammatory activity, can significantly inhibit the production

Fialuridine (DRG-0098) is a DNA-directed DNA polymerase inhibitor potentially for the treatment of HBV infection with potent activity against hepatitis B virus in vitro and in vivo.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Zelpolib is a specific inhibitor of DNA polymerase δ (Pol δ), thereby inhibiting DNA replication and DNA double-strand break homologous recombination repair. It exhibits antiproliferative activity in triple-negative breast cancer cell lines, pancreatic cancer cell lines, and platinum-resistant pancreatic cancer cell lines.

Aphidicolin, an antibiotic derived from the mold Cephalosporium aphidicola, is a potent inhibitor of DNA (deoxyribonucleic acid) synthesis, effectively hindering the proliferation of herpes simplex virus[2]. It targets DNA polymerase α and δ, disrupting mitotic cell division by affecting DNA polymerase activity[1]. Additionally, aphidicolin enhances apoptosis when combined with arabinosyl nucleosides in a human promyelocytic leukemia cell line[3].

PMEG-DP disodium is an effective inhibitor of DNA polymerase (IC50=2.5 μM), exerting strong inhibitory effects particularly on DNA polymerases α and δ. As the active metabolite of GS-9191, it efficiently impedes the growth of cell lines infected with human papillomavirus (HPV). PMEG-DP disodium is useful in research related to HPV-associated diseases.

Delavirdine mesylate (BHAP-U 90152 (mesylate)) is a non-nucleoside reverse transcriptase inhibitor (NNRTI).

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine is part of Highly Active Antiretroviral Therapy (HAART), which can be used to treat human immunodeficiency virus (HIV) type 1.

T2AA, a proliferating cell nuclear antigen (PCNA) inhibitor, disrupts protein-protein interactions between PCNA and both a PIP-box-containing peptide (IC50= 1 μM) and full-length p21, reducing cellular colocalization of PCNA with DNA polymerase δ. This compound effectively inhibits DNA replication and cell proliferation in U2OS and HeLa cells in a concentration-dependent manner, additionally inducing S phase cell cycle arrest at a 20 μM concentration. Furthermore, T2AA enhances DNA double strand break formation alongside cisplatin in a neutral comet assay and augments cisplatin-induced reductions in clonogenic survival in HeLa and U2OS cells.