DNA/RNA Synthesis

<p>BMH-22 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.</p>

<p>Phen-DC3 is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases (IC50s of 65±6 and 50±10 nM, respectively).</p>

<p>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′-</p>

<p>Werner syndrome RecQ helicase-IN-4 is a WRN inhibitor with anticancer and anti-proliferative activity, used in colorectal and gastric cancer research.</p>

<p>DDD100097 is a N-myristoyltransferase inhibitor with potential inhibitory effects on Trypanosoma brucei, which can be used to study neurological disorders.</p>

<p>CM03 is a cell-selective G-quadruplex ligand with anti-cancer activity, stabilizing G4 genes, useful in pancreatic cancer research.</p>

<p>AS-136A is an orally active MV RdRp inhibitor with antiviral activity that inhibits measles virus and blocks viral RNA synthesis.</p>

<p>Nitracrine: a 1-nitroacridine, hypoxia-selective, anti-tumor agent; inhibits RNA synthesis, binds DNA reversibly and forms covalent adducts.</p>

<p>Laromustine (VNP40101M) is a sulfonyl hydrolysis alkylation prodrug for cancer treatment with significant anticancer activity, inhibiting thioredoxin reductase.</p>

<p>10-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor.</p>

<p>CID 5951923 is an inhibitor of KLF5 transcription factor with an IC50 of 603 nM.</p>

<p>CGP 53353 (DAPH-7) is a PKC inhibitor with inhibitory effects on PKCβII and PKCβI and can be used to study atherosclerosis.</p>

<p>Synucleozid is a potent the SNCA mRNA inhibitor that encodes α-synuclein protein (IC50=1.5 μM), has the potential for the investigation of Parkinson’s disease.</p>

<p>Glucocorticoid receptor modulator 1 is a orally NF-κB and AP-1 inhibitor, inflammatory factors IL-6, IL-1β, TNF-α, and MMP-13, alleviating skin inflammation.</p>

<p>Bofumustine is a chloroethyl nitrosourea with anti tumor properties.</p>

<p>BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor (IC50: ~0.2 μM) with anticancer activities.</p>

<p>Potent WRN inhibitor, Werner syndrome RecQ helicase-IN-3, is orally active with 0.06 µM IC50; exhibits antiproliferative and anticancer effects.</p>

<p>Crisnatol, a potent and selective DNA intercalator, has potential anticancer activity.</p>

<p>2-Fluoroadenine (NSC-27364) has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for anticancer studies.</p>

<p>1,2,3,5-Tetra-O-acetyl-D-xylofuranose is a starting material for the synthesis of nucleosides.</p>

<p>HBV-IN-16, a quinoline derivative, inhibits HBV cccDNA, key for viral replication (from patent WO2019121357A1).</p>

<p>GW8510 is a CDK2 and RRM2 inhibitor that affects DNA synthesis and antiproliferation in tumor cells. In mammalian aging models, GW851 prolongs lifespan.</p>

<p>REV7/REV3L-IN-1 is a inhibitor of REV7/REV3L interaction(IC50 of 78 μM),</p>

<p>AB-182 is an aziridine derivative with antitumor activity.</p>

<p>BPIC is an agent of anti-tumor that acts by inhibiting inflammation and scavenging free radicals.</p>

<p>HBV-IN-22 (Compound LC5f) is an HBV DNA replication inhibitor that acts on both wild-type HBV (IC50: 0.71 μM) and drug-resistant HBV (IC50: 0.84 μM).</p>

<p>BRACO19 3HCl inhibits telomerase, blocking its capping function, and prevents HAdV viral replication.</p>

<p>UIAA-II-232 (compound 19b) is a potent inhibitor of DNA gyrase catalytic (IC 50= 3.5 μM).</p>

<p>Datelliptium chloride is a DNA-intercalating agent derived from ellipticine. Datelliptium chloride shows anti-tumor activities.</p>

<p>RHI002-Me is a methylated derivative of RHI002, a selective inhibitor of human RNaseH2.</p>

<p>Antitumor agent-84 stabilizes G-quadruplex DNA, exhibits potent anti-tumor effects.</p>

<p>HIV-1 Inhibitor-43 suppresses HIV-1, with EC50: 21.3 nM (Y188L), 6.2 nM (K103N-Y181C), &lt;0.7 nM (K103N/Y181C), and lowers HIV RNA/p24 protein.</p>

<p>HIPP is a highly selective inhibitor of antineoplastic CtBP.</p>

<p>IDD388 is a selective and potent aldose reductase (ALR2) inhibitor with antitumor activity that inhibits the ALR1 receptor.</p>

<p>Cylindrospermopsin: a toxic cyanobacterial uracil derivative, disrupts protein/glutathione synthesis in hepatocytes, and is genotoxic.</p>

<p>EGFR/HER2/TS-IN-2: Strong EGFR, HER2 &amp; TS inhibitor; EGFR IC50=0.173μM, HER2 IC50=0.125μM, TS IC50=1.12μM; kills MDA-MB-231 cells (IC50=1.69μM).</p>

<p>FLDP-5: BBB-penetrant curcuminoid, induces ROS, DNA damage, S phase arrest, suppresses tumors in LN-18 cells.</p>

<p>BAY-707: tolerable in mice, no anticancer efficacy; potent, selective MTH1 inhibitor, IC50 = 2.3 nM; good PK profile.</p>

<p>15(S)-HpETE is a product of arachidonic acid formed in the 15-lipoxygenase pathway and inhibits angiogenesis.</p>

<p>HBV-IN-21 inhibits HBV DNA replication (IC50: 2.2 μM) and binds HBV capsid protein well (KD: 60.0 μM).</p>

<p>CAY10760 inhibits RAD51-BRCA2 interaction (EC50=19 μM), reduces homologous recombination by 54%, and hinders BxPC-3/Capan-1 cancer cell proliferation.</p>

<p>360A iodide is a selective stabilizer of G-quadruplex and inhibits telomerase activity (IC50: 300 nM in TRAP-G4 assay).</p>

<p>ERCC1-XPF-IN-1: potent ERCC1-XPF inhibitor (IC50: 0.49 μM), hampers CPD removal, boosts UV toxicity, hinders DNA repair.</p>

<p>BMH-23 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.</p>

<p>cp028 inhibits pre-mRNA splicing in vitro.</p>

<p>Halofuginone specifically inhibits collagen type I and MMP-2 gene expression, which may result in the suppression of angiogenesis and tumor cell growth.</p>

<p>Enocitabine is a nucleoside analog.</p>

<p>IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes.</p>

<p>5,10-Dideazaaminopterin is an antileukemic drug.</p>

<p>HBV-IN-14: a pyridinopyrimidinone, potent cccDNA inhibitor for HBV study (patent WO2021190502A1, comp 5).</p>

<p>MMV688845: NTM RNA polymerase inhibitor, kills Mycobacterium abscessus, and fights TB.</p>

<p>CB 3717 is an enzyme inhibitor, antineoplastic agent, folic acid antagonist.</p>

<p>NPD9948 is a competitive inhibitor of MTH1.</p>

<p>BMVC2 (o-BMVC), a carbazole derivative of BMVC, is a G-quadruplex (G4) stabilizer.</p>

<p>Antitumor agent-85 stabilizes G4-DNA with potent anti-tumor effects.</p>

<p>CBL0100 is an inhibitor of viral transcriptional elongation, blocking both HIV-1 replication and reactivation.</p>

<p>Antibacterial agent 124 inhibits Sa ProRS with an IC50 of 0.18 μM.</p>

<p>NSC666715 is the strand-displacement activity of DNA polymerase inhibitor.</p>

<p>HBV-IN-15, a flavone derivative, is a potent cccDNA inhibitor, potentially aiding HBV research.</p>

<p>ML372 is a potent and selective SMN Modulator (EC50 = 12 nM, 325% increase inSMN2) with good potency, pharmacokinetics, tolerance, and CNS penetration.</p>

<p>Fozivudine tidoxil, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

<p>6-Hydroxy-DOPA is an allosteric inhibitor of RAD52, it inhibits proliferation of BRCA-deficient cancer cells in vitro and also inhibits APE1.</p>

<p>Cytembena is a cytostatic and a carcinogenic compound that may increase the incidence of fibroadenomas.Cytembena broadly inhibits DNA biosynthesis.</p>

<p>SMN-C2, a SMN2 gene splicing regulator, is an RNA-binding ligand that regulates pre-mRNA splicing and has potential for studying spinal muscular atrophy.</p>

<p>Galocitabine (Neofrutulon), a thymidylate synthase inhibitor, is used potentially for the treatment of cancer.</p>

<p>D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM.</p>

<p>CHD1Li 6.11 inhibits CHD1L protein (IC50: 3.3 µM), shrinks CRC tumors in vivo, and is orally active.</p>

<p>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</p>

<p>ERCC1-XPF-IN-2: Nucleotide repair active, boosts cisplatin, inhibits ERCC1-XPF (IC50: 0.6 μM).</p>

<p>116-9e (MAL2-11B) is an Hsp70 chaperone DNAJA1 inhibitor with antiviral properties, inhibits SV40 replication, and can be used to study cancer drug resistance.</p>

<p>TTP-8307 is an antiviral compound that inhibits the replication of rhinoviruses and enteroviruses and is used in the study of viral infections.</p>

<p>Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide can be used in anticancer studies.</p>

<p>ZIM, from 4-Aminoantipyrine, induces DNA and chromosomal damage, cell death, and phagocytosis, with potential in cancer therapy.</p>

<p>RP-6685 is a potent, selective DNA Polθ inhibitor with strong oral efficacy, an IC50 of 5.8 nM, and marked antitumor effects in mice.</p>

<p>Anticancer agent 73 inhibits TRBP, disrupting TRBP-Dicer, and hinders HCC growth and spread by altering HCC miRNA and protein expression.</p>

<p>DDRI-18 is an inhibitor that regulates the DNA damage response, has anticancer activity, and inhibits non-homologous end-joining (NHEJ) DNA repair.</p>

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

<p>DNA polymerase-IN-3 (Compd 5b), a coumarin derivative, demonstrates inhibitory activity against Taq DNA polymerase and has potential applications in</p>

<p>Votoplam functions as a gene splicing modulator, employed in the inhibition of Huntington's disease [1].</p>

<p>5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor and other folate related enzymes inhibitor.</p>

<p>5,11-methenyltetrahydrohomofolate blocks GAR &amp; AIR transformylase; used as an anti-purine drug.</p>

<p>Diazoketone methotrexate is an analog of methotrexate with potential antitumor activity.</p>

<p>WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).</p>

<p>TAS-114 is a dUTPase and DPD inhibitor that modulates catabolic pathways to improve systemic availability of 5-FU.</p>

<p>UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.</p>

<p>BVDU 5′-Triphosphate is an antiviral agent labeled with 5′-Triphosphate that specifically targets viral DNA polymerase.</p>

<p>WRN Inhibitor 1 (example 7) is an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN), selectively targeting its helicase domain.</p>

<p>8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.</p>

<p>9-Deazaguanine is a nucleoside analogue exhibiting inhibitory activity against bovine purine nucleoside phosphorylase (PNP).</p>

<p>53BP1-binding protein 1 (53BP1) engages with dimethylated lysine 20 on histone 4 (H4K20me2) through its tandem tudor domains within a homodimer configuration, crucial for the DNA damage response. UNC2170, a micromolar 53BP1 ligand, selectively interacts with this site, demonstrating at least 17-fold preference for 53BP1 over similar proteins. This interaction occurs in a pocket formed by the 53BP1's tudor domains. Moreover, UNC2170 acts as an antagonist to 53BP1 in cellular lysates, effectively inhibiting class switch recombination, a process dependent on the functional 53BP1 tudor domain, thus confirming its cellular activity.</p>

<p>DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor with an IC50 value of 48 μM.</p>

<p>Pen is an oral cancer drug that blocks DNA synthesis by inhibiting key enzymes and integrating into DNA.</p>

<p>COH1 is a ribonucleotide reductase (RR) inhibitor utilized in research pertaining to cancer, mitochondrial diseases, and neurodegenerative disorders [1].</p>

<p>WRN Inhibitor 2 (example 118), a potent inhibitor of the WRN (Werner Syndrome ATP-dependent helicase enzyme), exhibits a pIC50 value of 7.0 or greater [1].</p>

<p>H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) with an IC50 of approximately 10 nM, effectively targeting its helicase, ATPase, and exonuclease</p>

<p>AVG-233 is an RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity for the study of respiratory syncytial virus infections.</p>

<p>hDHODH-IN-1 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an anti-inflammatory effect.</p>

<p>RNA polymerase II-IN-1 (19iv), an amatoxin, inhibits Pol II at 36.66 nM IC50, is more toxic to cancer cells, less to normal cells than α-Amanitin.</p>

<p>DHX9-IN-6 is a highly effective ATP-dependent RNA helicase A (DHX9) inhibitor, used in cancer research.</p>

<p>DHX9-IN-4 is an ATP-dependent RNA helicase DHX9 inhibitor used in cancer research.</p>