DNA/RNA Synthesis

Phelorphan is an inhibitor of enkephalinase.

TDRL-551 is a novel and potent replication protein A (RPA) inhibitor (IC50=18 µM) with potential anticancer activity.TDRL-551 inhibits RPA-DNA interaction and

Piposulfan, a water-insoluble alkylating agent, is used as an antineoplastic and anti-tumor agent.

Yoshi-864, an alkyl sulfonate, alkylates DNA to hinder replication; potential anti-cancer agent.

Nitracrine dihydrochloride is an acridine antineoplastic agent used in mammary and ovarian tumors. It inhibits RNA synthesis.

R-82913 blocks RNA-polymerase, lowers mouse DOI-head-shakes, halts 13 HIV-1 strains with 0.15µM IC50, beats AZT-TP by 20x; ineffective on HIV-2.

UCK2 Inhibitor-1 is a non-competitive UCK2 inhibitor with an IC 50 of 4.7 µM .

RTC14 induces PTC readthrough, restoring dystrophin and aiding muscle function in Duchenne model mice.

12(S)-HpETE activates human blood leukocyte 5-LOE and mediates induction of c-fos and c-jun, activation of AP-1, and endothelium-dependent vasoconstriction.

Photoregulin3 is a inhibitor of rod photoreceptor gene expression, potentially though Nr2e3 modulation.

Valomaciclovir is a DNA polymerase inhibitor potentially for treatment of acute herpes zoster and EB virus infection.

ATB107 is a potent and novel inhibitor of indole-3-glycerol phosphate synthase (IGPS, KD: 3 μM).

Remdesivir (GS-5734) is a broad-spectrum antiviral prodrug effective against SARS-CoV-2 and Ebola, used for research, not human treatment.

POLA1 inhibitor 1: oral, antitumor, effective on various cancers and Adaroten-resistant cells.

Teloxantrone, a DNA topoisomerase II inhibitor, is used potentially for the treatment of solid tumors.

BAY-707: potent, selective MTH1 inhibitor with excellent engagement and pharmacokinetics but no anticancer efficacy alone or combined.

Ametantrone Acetate is a topoisomerase II inhibitor of anthrapyrazole family, which can lead to DNA covalent crosslinking.

RECQL5-IN-1, an oral RECQL5 inhibitor (IC50 46.3 nM), targets enzyme/non-enzyme domains, useful in breast cancer research.

Teloxantrone: an anthrapyrazole antibiotic inhibiting DNA replication, RNA/protein synthesis by interacting with DNA and topoisomerase II.

Chlorozotocin is a nitrosourea. It is used for cancer therapy.

CB 3731 is used in fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase.

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation ( IC 50 =1 μM), does not blocking basal

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

CID 5951923 is an inhibitor of KLF5 transcription factor with an IC50 of 603 nM.

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.

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

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

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

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

10-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor.

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

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

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

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM.

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

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

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.

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

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

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.

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

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.

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

GNE-371 is a probe for human transcription initiation factor TFIID subunit 1 and transcription initiation factor TFIID subunit 1-like second bromodomain.

Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the

Cytarabine 5′-monophosphate (ara-CMP), an active metabolite of the nucleoside analog cytarabine formed by deoxycytidine kinase, is incorporated into DNA by DNA polymerase α, significantly slowing DNA synthesis. It inhibits nuclear and mitochondrial DNA replication in S. cerevisiae at 15 mM and improves survival in an L1210 murine leukemia model at 3.5-75.1 mg/kg.

Abetimus (LJP 394 free base), an immunosuppressant composed of four double-stranded DNA (dsDNA) oligonucleotides, can crosslink anti-dsDNA antibodies on B cell

(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.

PTC258 is a specific, orally active modulator of the splicing of the Elongator complex protein 1 gene (ELP1), enhancing its expression both in vitro and in vivo

MOMA-341, ATP-competitive WRN allosteric inhibitor (Cys727 site), induces DNA damage and tumor regression in dMMR/MSI-H models, for solid tumors.

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

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

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

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

SJ26 is a Wnt1 inhibitor known for its anticancer activity. It inhibits the expression of WNT1 and the downstream signaling pathways mediated by WNT1 in a G-quadruplex structure-dependent manner, thereby suppressing the migratory activity of cancer cells.

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

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

Diazoketone methotrexate is an analog of methotrexate with potential antitumor activity.

5,11-methenyltetrahydrohomofolate blocks GAR & AIR transformylase; used as an anti-purine drug.

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

Emzadirib (RAD51-IN-2) is a potent RAD51 inhibitor with potential anticancer activity for the study of DNA damage repair.

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].

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

FAICAR (5-Formamidoimidazole-4-carboxamide ribotide), a purine nucleotide, plays a crucial role in metabolic processes.

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

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.

12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX.

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

RAD51-IN-4, a potent RAD51 inhibitor, may be useful in researching mitochondrial defect-related conditions.

Balapiravir HCl, an NS5B inhibitor, is used potentially for the treatment of HCV infection.

G4/HDAC-IN-1, a G4/HDAC dual inhibitor, IC50 1.1 µM, blocks TNBC growth, useful in cancer research.

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

8-NH2-ATP tetrasodium, an inactive ATP variant, originates from 8-NH2-Ado tetrasodium, which triggers the apoptosis-associated cleavage of poly (ADP-ribose) polymerase [1] [2].

KY386 is a potent and selective DHX33 helicase inhibitor with an IC50 value of 19 nM.

WRN Inhibitor 5 (Example 157), a cyclic vinyl sulfone-based compound, serves as an inhibitor of Werner Syndrome ATP-dependent helicase enzyme (WRN).

NVS-SM2 boosts SMN2 splicing, enhances exon 7 inclusion, and raises SMN protein levels orally.

3-Cyanovinylcarbazole phosphoramidite: an antiviral, hinders viral DNA synthesis, modifies ribonucleotides.

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

MC-VC-PAB-Cyclohexanediamine-Thailanstatin A is a spliceostatin analog and a drug-linker conjugate for antibody-drug conjugates (ADC), comprising the cytotoxic

WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).