5-Formylindole-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Tubercidin (7-Deazaadenosine) is an adenosine analog, is an antibiotic obtained from Streptomyces tubercidicus.Target: AntibacterialTubercidin inhibits the growth of Streptococcus faecalis by 50 % at a concentration of 20 nM. Tubercidin is not subject to cleavage by adenosine phosphorylase or to deamination by adenosine deaminase. The antibiotic served as a substrate for numerous enzymes involved in the anabolism of adenosine, as demonstrated by its incorporation into RNA and DNA, and by the formation of nicotinamide-deaza-adenine dinucleotide. Tubercidin proves to be a weak inhibitor of adenosine phosphorylase, and interfered with the phosphorylation of adenosine and AMP. The inhibition of the growth of S. faecalis by Tubercidin is prevented by purine and pyrimidine nucleosides, ribose 5-phosphate, pyruvate, and certain amino acids. In the presence of Tubercidin, growing cultures of the test organism used pyruvate instead of glucose, whereas in the absence of the antibiotic glucose served as the main source of energy. It is suggested, therefore, that the impairment of growth is due primarily to the interference of Tubercidin with the utilization of glucose.
5-Propargylamino-ddUTP, a nucleoside molecule that can be used to synthesis of cyanine dye-nucleotide conjugate which is used in nucleic acid labeling or sequence analysis[1].
Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic[1].
Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area[1][2].
m7Gpppm6AmpG is a trinucleotide mRNA 5’ cap analogs. m7Gpppm6AmpG can be used for RNA synthesis in vitro[1].
Foscarnet sodium (Trisodium phosphonoformate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet sodium is an antiherpesvirus agent used in cytomegalovirus retinitis[1][2][3].
4-Methoxyestradiol is methoxylestradiol that induces oxidative DNA damage in human lung epithelial cells. 4-Methoxyestradiol also elevates ROS and SOD activities in H1355 cells[1].
2-O-Methylcytosine, an O-alkylated analogue a DNA adduct, is the damaged nucleobase[1].
DMT-dC(bz) Phosphoramidite is typically used in the synthesis of DNA[1].
DNA Gyrase-IN-5 (Compound 8I-w) is a potent DNA gyrase inhibitor with an IC50 of 0.10 μM. DNA Gyrase-IN-5 shows antibacterial activities against wild type and drug-resistant strains[1].
5'-O-DMT-2'-O-TBDMS-Ac-rC is a modified nucleoside and can be used to synthesize DNA or RNA.
Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of drug, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription[1][2].
DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity[1].
Capecitabine is an oral prodrug that is converted to its active metabolite, fluorouracil (FU), by thymidine phosphorylase.
AT-130 is a potent inhibitor of HBV capsid assembly, inhibits wild-type HBV replication with IC50 of 2.4 uM; inhibits replication of wild-type and lamivudine-resistant strains of hepatitis B virus in vitro with same sensitivity (rtL180M, rtM204I, and rtL180M + rtM204V); blocks HBV replication at the level of viral RNA packaging, interferes with capsid morphogenesis, shows activity against the main lamivudine- and adefovir-resistant mutants.
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis[1].
ddATP (2',3'-Dideoxyadenosine 5'-triphosphate) trisodium, an active metabolite of 2',3'-dideoxyinosine, is a chain-elongating inhibitor of DNA polymerase. ddATP trisodium can be used for Sanger method for DNA sequencing and research of virus infection[1][2][4].
E3330 (APX-3330) is a direct, orally active AP endonuclease 1 (APE1; also known as REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration[1-4].
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis[1].
Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA)[1].
DNA polymerase-IN-3 (Compd 5b) is a coumarin derivative that exhibits inhibitory activity against Taq DNA polymerase and can be used in proliferative disease research[1].
DHODH-IN-16 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.396 nM for human DHODH[1].
Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer[1][2].
DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor, IC50: 48 μM. DMA-IN-1 inhibits Caulobacter growth with an MIC of 35 μM[1].
ML216(CID-49852229) is a potent inhibitor of the DNA unwinding activity of BLM helicase; showing similar IC50s of 3.0 and 0.97 μM for full length BLM and BLM636–1298 respectively.IC50 value: 3.0/0.97 uM(Full length/636–1298 BLM)Target: BLM helicase inhibitorML216 shows cell-based activity, and can induce sister chromatid exchanges, enhance to the toxicity of aphidicolin and exert anti-proliferative activity in cells expressing BLM, but not in those lacking BLM.
TDRL-X80 is a potent inhibitor of xeroderma pigmentosum group A (XPA) protein. TDRL-X80 inhibits XPA’s DNA binding activity. TDRL-X80 exhibits activity against single, double, and Cisplatin-damaged DNA with IC50s of 18, 20, and 29 μM in fluorescence polarization (FP) analyses , and with IC50s of 21, 39, and 28 in ELISA Analysis[1].
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity[1]. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells[2].