polymerase

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.

RNA polymerase II-IN-2 (compound 20iii), a potent inhibitor of RNA polymerase II (Pol II) with a K i value of 9.5 nM, demonstrates cytotoxicity against cancer cells, exhibiting toxicity levels 2 and 5 times higher than α-amanitin in CHO and HEK293 cells, respectively [1].

T7 RNA polymerase, expressed by Escherichia coli from the T7 bacteriophage RNA polymerase gene, is a highly specific enzyme utilized for in vitro transcription (IVT) of mRNA. This polymerase requires Mg 2+ and selects only DNA templates that contain the T7 promoter sequence, whether single-stranded or double-stranded. It employs NTPs to synthesize RNA that is complementary to the single-stranded DNA following the promoter [1] [2].

RNA polymerase II-IN-1 (compound 19iv), an amatoxin, selectively inhibits RNA polymerase II (Pol II) with an IC50 of 36.66 nM. It exhibits heightened cytotoxicity towards cancer cells and reduced toxicity in normal cells compared to α-Amanitin [1].

DNA polymerase-IN-4 (Compd 5c), a coumarin derivative, exhibits antiretroviral activity, achieving an IC50 of 134.22 μM [1].

Taq DNA polymerase is a thermostable enzyme utilized in polymerase chain reactions (PCR) to amplify DNA sequences [1].

Poly(A) polymerase enzymatically adds a polyadenosine tail of 20-200 adenine bases to the 3' end of RNA, a process that involves integrating ATP as AMP. This modification enhances RNA stability and augments mRNA translation efficiency in eukaryotic cells, evidencing the enzyme's high tailing efficiency [1] [2].

DNA polymerase-IN-2 (Compd 3c), a coumarin derivative, demonstrates inhibitory activity towards Taq DNA polymerase, with an IC50 value of 48.25 μM, and holds potential for application in value-added disease research [1].

DNA polymerase-IN-3 (Compd 5b), a coumarin derivative, demonstrates inhibitory activity against Taq DNA polymerase and has potential applications in proliferative disease research [1].

Viral polymerase-IN-1 hydrochloride, a derivative of Gemcitabine, effectively inhibits influenza A and B virus infections, demonstrating IC90 values ranging from 11.4 to 15.9 μM, and possesses activity against SARS-CoV-2 infection. This compound acts by interfering with viral RNA replication/transcription within cells [1].

Remdesivir (GS-5734) is a nucleoside analog, a broad-spectrum antiviral compound that exerts its activity by inhibiting the RNA-dependent RNA polymerase of viruses. Remdesivir is active against Ebola, SARS, and MERS viruses, and is potentially therapeutic against COVID-19.

Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis.

RBN012759, a potent and selective PARP14 inhibitor, decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1 PARP2 (IC50=5 1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

Favipiravir (T-705) (T-705), an effective and selective RNA-dependent RNA polymerase inhibitor, are applied to treat influenza virus infections.

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.

3-Aminobenzamide (PARP-IN-1) is an effective inhibitor of PARP (IC50<50 nM in CHO cells) and a mediator of oxidant-induced myocyte dysfunction during reperfusion.

Filibuvir (PF-00868554) is a selective and noncovalent inhibitor of HCV NS5B RNA-dependent RNA polymerase. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM.

Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) possesses anti-angiogenic, anticonvulsive, anti-inflammatory, anti-oxidant, neuroprotective, and anti-nociceptive activities. Vanillyl alcohol can effectively inhibit the cytotoxicity and improved cell viability in 1-methyl-4-phenylpyridinium (MPP+)-induced MN9D dopaminergic cells, it also can attenuate the elevation of reactive oxygen species (ROS) levels, decrease in the Bax/Bcl-2 ratio and poly (ADP-ribose) polymerase proteolysis.

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

Acyclovir (Aciclovir) is a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses of the herpesvirus family.

VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.

JTK-109 is an inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor and inhibits G1b and G3a subgenomic replicons and recombinant enzymes.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

GS-6620 PM is a derivative of GS-6620, an orally administered anti-hepatitis C virus polymerase inhibitor and a novel potent C-nucleoside adenine analogue monophosphate prodrug.GS-6620 has limited activity against other viruses and maintains only partial activity against the closely related bovine viral diarrhea virus (EC50, 1.5 μM).

BILB-1941 (BILB-1941ZW) is an inhibitor of HCV NS5B polymerase and can be used in studies about HCV infection.

2’-beta-C-Methyl inosine (2’-C-Methylinosine) is an HCV RNA polymerase inhibitor with antiviral activity and is being studied for the treatment of hepatitis C virus infection.

ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

2'-Hydroxychalcone is a drug synthesis intermediate for the synthesis of flavonoids. 2'-Hydroxychalcone loaded in nanoemulsion showed fungicidal activity against Coccidioides parapsilosis in Danio rerio model.2'-Hydroxychalcone induced cytotoxicity through oxidative stress in lipid-loaded Hepg2 cells.2'-Hydroxychalcone inhibited the induction of ICAM-1, VCAM-α, tumor necrosis factor-α, and tumor necrosis factor-alpha as determined by reverse transcription-polymerase chain reaction determined by tumor necrosis factor-alpha induces steady-state transcript levels of ICAM-1, VCAM-1, and E-selectin, and therefore may interfere with the transcription of their genes.

N4-Benzoyl-2′-deoxycytidine is a synthetic nucleoside analog of the natural nucleoside deoxycytidine (dC), a competitive inhibitor of DNA polymerase. In vitro studies have shown that it inhibits replication in viruses, bacteria and eukaryotic cells. It has also been shown to inhibit tumor cell growth in animal models.

GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which penetrates the skin and is metabolized in the epithelium to an active nucleoside triphosphate analogue.GS-9191 has antiproliferative activity and reduces the size of papillomas in a dose-related manner.GS-9191 may be useful in the treatment of HPV-induced lesions.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.

TMC647055 Choline Hydroxide Salt is a novel and potent non-nucleoside inhibitor of the HCV NS5B polymerase which potentially for the treatment of HCV infection. It has nanomolar cellular potency (EC(50) of 82 nM) with minimal associated cell toxicity (CC(

8-CHLOROQUINAZOLIN-4(1H)-ONE is inhibitor of Poly [ADP-ribose] polymerase 1 (human)

Setrobuvir (ANA-598) is an orally active non-nucleoside HCV NS5B polymerase inhibitor with inhibitory effects on de novo RNA synthesis and primer extension with IC50s between 4 and 5 nM. setrobuvir shows good binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp.

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX. VPC-70063 exhibits Myc-Max transcriptional activity inhibition of 106% with an IC50 of 8.9 μM and Myc-Max/UBE2C downstream pathway inhibition of 94%. VPC-70063 can be used for studies about anticancer.

Talviraline (Bay 10-8979) is an RNA-induced DNA polymerase inhibitor.Talviraline is a potent inhibitor of HIV-1-induced cell killing and HIV-1 replication in a variety of human cell lines, as well as in fresh human peripheral blood lymphocytes and macrophages.

Totrombopag (SB559448) is a candidate compound for action on RSV polymerase.

Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.

ddATP is a dideoxynucleotide, used as a chain extension inhibitor for DNA polymerase, and used for DNA sequencing by the Sanger method.

Uprifosbuvir (MK-3682) is a uridine nucleoside monophosphate prodrug inhibitor of hepatitis C virus NS5B RNA polymerase with antiviral activity for the study of chronic hepatitis C virus.

Galidesivir is a viral RNA-dependent RNA polymerase (RdRP) inhibitor and broad spectrum antiviral nucleotide.In vitro, galidesivir displays antiviral activity against a range of RNA viruses, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses, and flaviviruses (EC50values range from 3 μM to >100 μM). Galidesivir protects against Ebola and Marburg viral infection in animal models.

AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).

TMC-649128 PM is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC(50) value of 1.2 muM and showing moderate in vivo bioavailability in rat (F=14%).

Niraparib metabolite M1 is niraparib metabolite, niraparib is a novel poly(ADP-Ribose) polymerase (PARP) inhibitor.

IDX184 is a potent, orally active, targeted HCV polymerase inhibitor and nucleoside polymerase.IDX184 effectively inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM). IDX184 is a liver-targeted nucleotide prodrug with anti-HCV activity that inhibits HCV NS5B polymerase and can be used in combination with pegylated interferon-α2a and ribavirin for the primary treatment of chronic hepatitis C. It has been shown to inhibit HCV polymerase and nucleoside polymerase.

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of the mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression. This action confers it with anti-tumor properties.

PARPYnD is a potent photoaffinity probe for poly(ADP-ribose) polymerase (PARP) (IC50 values for PARP2, PARP1 and PARP6 are 6, 38 and 230 nM, respectively). PARPYnD labels PARP1 and PARP2 in the cell when an N3 functionalized fluorescent probe is attached and can inhibit isolated PARP6.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.