Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis[1].
5-Methylcytidine 5′-triphosphate (5-Methyl-CTP) is a modified nucleoside triphosphates. 5-Methylcytidine 5′-triphosphate can apply in replacing unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells[1].
2'-F-Bz-dC Phosphoramidite can be used in the synthesis of oligoribonucleotides[1].
Thymidine-13C-1 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Remdesivir is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for ARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells.
N-Trityl-morpholino-T-5'-O-phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
DENV-IN-5 (Compound 4b) is a dengue virus (DENV) inhibitor with EC50s of 1.47, 9.23, 7.08 and 8.91 μM against DENV-I ∼ IV replication, respectively. DENV-IN-5 also inhibits HIV-1IIIB strain with an EC50 of 0.1512 μM[1].
Enoxacin-d8 (AT 2266-d8) is the deuterium labeled Enoxacin. Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing[1][2][3][4].
Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity[1][2].
5'-O-TBDMS-N2-ibu-dG is a nucleoside derivative and can be used for lead compounds synthesis with anti-bovine viral diarrhea virus activity[1].
Emetine hydrochloride, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine hydrochloride inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine hydrochloride potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect[1][2][3][4].
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].
Actinomycin D inhibits DNA repair with an IC50 of 0.42 μM.
Carbazole-d8 is the deuterium labeled Carbazole (HY-D0204). Carbazole is a tricyclic aromatic heterocyclic. Carbazole can form a new type of DNA minor groove complex to suppress the synthesis of new DNA or RNA[1][2].
1-Decarboxy-3-oxo-ceanothic acid is an anticancer agent. 1-Decarboxy-3-oxo-ceanothic acid inhibits DNA synthesis. 1-Decarboxy-3-oxo-ceanothic acid induces Apoptosis[1].
DMT-dT Phosphoramidite-13C10,15N2 is the 13C and 15N labeled DMT-dT Phosphoramidite[1]. DMT-dT Phosphoramidite is typically used in the synthesis of DNA[2].
Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4][5].
N2-Methylguanine is a modified nucleoside. N2-Methylguanine is an endogenous methylated nucleoside found in human fluids.
Risdiplam is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.
FAICAR (5-Formamidoimidazole-4-carboxamide ribotide) is a purine nucleotide.
DMT-2'-F-dA(bz) phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
3'-TBDMS-ibu-rG Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Deoxythymidine-5'-triphosphate-13C10,15N2 (dTTP-13C10,15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43[1].
Remdesivir nucleoside monophosphate is a metabolite of Remdesivir[1]. Remdesivir is a nucleoside analogue with effective antiviral activity against SARS-CoV and MERS-CoV[2].
DHODH-IN-5 is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor, with a pIC50 of 7.8 for human recombinant DHODH. DHODH-IN-5 inhibits measles virus replication, with a pMIC50 of 8.8[1].
Caracemide (NSC-253272) is a novel anticancer agent derived from a hydroxamic acid. Caracemide inactivates R1 by covalent modification at the substrate-binding site and inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide has demonstrated to produce severe central nervous system (CNS) toxicity. Caracemide has a toxic metabolite, methylisocyanate (MIC), in vivo[1][2].
Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase[1]. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C[2].
CGP-53353 (DAPH-7) is an potent PKC inhibitor with IC50s of 0.41 mM and 3.8 mM for PKCβII and PKCβI, respectively. CGP-53353 can inhibit glucose-induced cell proliferation and DNA synthesis in AoSMC and A10 cells. CGP-53353 can be used for researching atherosclerosis of diabetic patients[1].
Adenine-13C is the 13C labeled Adenine[1]. Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis[2][3][4].