Synthèse ADN/ARN

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).

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

Crisnatol, a potent and selective DNA intercalator, has potential anticancer activity.

ST7612AA1: potent, oral HDAC inhibitor; reactivates HIV-1 latency; shows antitumor effects; may study malaria.

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

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

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

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

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

Ferristatin II (Direct Black 38 free acid) is a polysulphonated dye and promotes the degradation of transferrin receptor-1 in vitro and in vivo.

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

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.

PEITC-Cys: anticarcinogenic, antileukemic, inhibits DNA synthesis in HL60, P450 inhibitor.

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

8-Azido-ADP (disodium) is a covalent inhibitor of ADP/ATP exchange in mitochondria, causing irreversible inhibition in light.

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

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

CB 3717 is an enzyme inhibitor, antineoplastic agent, folic acid antagonist.

Antitumor agent-85 stabilizes G4-DNA with potent anti-tumor effects.

MTH1-IN-2 is an inhibitor of MutT homolog 1 (MTH1), with anti-tumor activity.

<p>SPC-839 is an IKK-2 Inhibitor with oral activity.</p>

MMV688845: NTM RNA polymerase inhibitor, kills Mycobacterium abscessus, and fights TB.

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.

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.

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

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

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.

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.

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.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

MOMA-341 is a highly selective inhibitor targeting the Werner RecQ-like helicase (WRN). It exerts a dual mechanism of allosteric regulation and ATP competitive inhibition by binding to the cysteine 727 site of the WRN protein. In mouse models with mismatch repair deficiency (dMMR) or high microsatellite instability (MSI-H), MOMA-341 can induce DNA damage, cell apoptosis, and promote tumor shrinkage. This compound exhibits significant anti-tumor activity and has potential application prospects in the study of advanced and metastatic solid tumors.

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

(±)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.

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

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

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.

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.

Amotosalen is a Dermatologic Agent.

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

pppApG serves as an initial substrate for the synthesis of vRNA (viral RNA) and cRNA (complementary RNA), with applications in influenza virus research [1].

Thymidine-5’-O-(α,β-methylene)diphosphate (TMP-CP), a hydrolytically stable derivative of TDP, functions as an inhibitor of thymidine kinase (Ki = 23 µM).

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].

PD 121373, a Benzothiopyrano-indazole, inhibits nucleic acid synthesis, equally affecting DNA/RNA.

NSC15520 is an RPA inhibitor that inhibits helical destabilization of double-stranded DNA oligonucleotides and can be used to study DNA damage repair.

Cytidine 3'-monophosphate, a ribonucleotide, results from the hydrolysis of cytidine 2',3'-cyclic monophosphate via RNase—a process that cytidine 3'-monophosphate itself inhibits. Additionally, it can be dephosphorylated to cytidine by 3'-nucleotidase.

CCT239065 is a novel, selective, and efficacious nanomolar pyridopyrazinone V600EBRAF and LCK inhibitor.

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

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

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

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

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.

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.

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