DNA Polymerases Inhibitor

Ganciclovir triphosphate disodium solution (100 mM ± 3 mM) (GCV-TP disodium) is a competitive DNA polymerase inhibitor and a metabolite of Ganciclovir (HY-13637). Ganciclovir triphosphate disodium solution (100 mM ± 3 mM) can replace Guanine-5'-triphosphate to terminate DNA chain extension, and mimics dGTP (HY-138616) to compete with mammalian DNA polymerases. Ganciclovir triphosphate disodium solution (100 mM ± 3 mM) can be used in research related to HSV infection, retinoblastoma, glioblastoma and colorectal cancer.

ddCTP trilithium solution (100 mM) is a chain-terminating dideoxynucleotide. ddCTP trilithium is a type of chain-terminating deoxynucleotide. ddCTP trilithium can be incorporated into the extension primer chain that lacks the 3'-hydroxyl group, thereby terminating primer extension, viral genome replication, and DNA synthesis. ddCTP trilithium can distinguish almost identical RNA through distinguishable extension products in primer extension inhibition experiments. ddCTP trilithium is the active metabolite of Zalcitabine (HY-17392), which can competitively inhibit HIV reverse transcriptase, terminate the synthesis of viral DNA chains, and thereby inhibit HIV replication.

Acyclovir triphosphate (Synonyms: AcycloGTP) sodium is a Acyclovir (HY-17422) derivative that competitively inhibits viral DNA polymerase by acting as an analog to deoxyguanosine triphosphate (dGTP). Acyclovir triphosphate (sodium) (100 mM) is an inhibitor of HIV-1 reverse transcriptase. Acyclovir triphosphate (sodium) (100 mM) causes termination of viral DNA synthesis.

BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC₅₀ of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC₅₀ of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities.

Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a K_i of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI).

Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC₅₀ values of 61 and 108 μM. Euscaphic acid induces apoptosis.

Foscarnet trisodium hexahydrate (Trisodium phosphonatoformate hexahydrate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet trisodium hexahydrate is an antiherpesvirus agent used in cytomegalovirus retinitis.

AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) tetraammonium is an active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate tetraammonium exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate tetraammonium also inhibits the DNA polymerase of HBV. AZT triphosphate tetraammonium activates the mitochondria-mediated apoptosis pathway.

3′-Deoxythymidine (2′,3′-Dideoxythymidine), a nucleoside analog, inhibits eukaryotic cellular and viral DNA polymerases, and inhibits retrovirus infection in some cells.

MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.

NSC639828 is a potent inhibitor of DNA polymerase α with an IC₅₀ of 70 μM. NSC639828 has high antitumor activity. NSC639828 has the potential for researching cancer disease.

PNR-7-02 is a dual Rev1 and human DNA polymerase η (hpol η) inhibitor, with an IC₅₀ value of 8 μM against hpol η. PNR-7-02 binds to hpol η to disrupt the orientation of template DNA and block the catalytic function of hpol η. When used in combination with Cisplatin (HY-17394), PNR-7-02 induces DNA damage and replication stress in cells with intact hpol η function. PNR-7-02 can be used in mechanism studies related to chronic myeloid leukemia and ovarian cancer.

5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABA_A receptors.

GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts.

SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC₅₀=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC₅₀=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors.

Polθ-IN-4 is an orally active prodrug of a DNA polymerase θ (Polθ) inhibitor with K_ms of 3.7, 3.7 and 5.2 μM in human, mouse and rat recombinant alkaline phosphatases. Polθ-IN-4 that inhibits Polθ activity by targeting its ATP-dependent helicase domain. Polθ-IN-4 demonstrates significant anti-tumor activity in multiple animal experiments. Polθ-IN-4 can be used for the studies of breast cancer and ovarian cancer.

1,4-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.

Polθ-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).

AZT 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.

AZT 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.