COH1 is a ribonucleotide reductase (RR) inhibitor. COH1 can be used in research into cancer, mitochondrial diseases, and neurodegenerative diseases[1].
Anticancer agent 73 (compound CIB-3b) is a anticancer agent, potently targeting TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. Anticancer agent 73 can rebalance the expression profile of oncogenic or tumor-suppressive miRNAs. Anticancer agent 73 suppresses the proliferation and metastasis of HCC in vitro and in vivo[1].
WRN inhibitor 1 (example 7) is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity. WRN inhibitor 1 has the potential to study cancer[1].
DMTr-FNA-C(Bz)Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect[1].
Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, 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].
Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii[1].
1-Hydroxyanthraquinone, a naturally occurring compound with oral activity from some plants like Tabebuia avellanedae, exhibits carcinogenic effect[1].
L189 is a novel human DNA ligase inhibitor, inhibits hLigI/III/IV with IC50 of 5/9/5 μM.IC50 value: 5/9/5 μM (for hLigI/III/IV)Target: DNA ligasein vitro: L189 is a competitive inhibitor with respect to nicked DNA. L189 inhibits DNA ligases I, III and IV in DNA joining assays with purified proteins and in cell extract assays of DNA replication, base excision repair and non-homologous end joinging. L189 markedly increases killing of HCT116 colon cancer cells and the other cancer cell lines by ionizing radiation.
Gemcitabine (NSC 613327;LY188011) is a DNA synthesis inhibitor which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively.
ddATP is a dideoxynucleotide, acts as a chain-elongating inhibitor of DNA polymerase, used for Sanger method for DNA sequencing[1].
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70[1][2].
Cylindrospermopsin is a cyanotoxin produced by a variety of freshwater cyanobacteria. It is a polycyclic uracil derivative containing guanidine and sulfate groups, which can inhibit protein synthesis and covalently modify DNA or RNA[1].
BVDU 5′-Triphosphate is an antivirus agent with 5′-Triphosphate label, targeting viral DNA polymerase. BVDU 5′-Triphosphate shows excellent selectivity against varicella-zoster virus (VZV) and herpes simplex virus type 1 (HSV-1), due to a specific phosphorylation by the virus-encoded thymidine kinase.
Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.
DNA Gyrase-IN-2 (Compound 22a) is a bacterial DNA gyrase B inhibitor with IC50s of 3.29-10.49 and 4.41-5.61 µM for E. coli DNA gyrase and M. tuberculosis DNA gyrase. Anti-tubercular and antibacterial activity[1].
Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth[1][2].
8-NH2-ATP, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado is reported to be potent as shown by induction of apoptosis-related cleavage of poly (ADP-ribose) polymerase[1][2].
Influenza A virus-IN-5 (Compound 16e) is a potent, orally active anti-influenza A virus (IAV) agent with an IC50 of 1.29 μM. Influenza A virus-IN-5 inhibits the transcription and replication of viral RNA with acceptable cytotoxicity[1].
TTP-8307 is a potent inhibitor of the replication of several Rhinoviruses and Enteroviruses, targets the nonstructural protein 3A, inhibits the replication of coxsackievirus B3 (CVB3 Nancy) with EC50 of 1.2 uM; 3A mutations V45A, I54F, and H57Y confer resistance to TTP-8307.
Streptolydigin (Portamycin) is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor with a Ki of 18 μM and a Kd of 15 μM. Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases[1][2][3]. Streptolydigin possess potent antibacterial activity, particularly against anaerobes and some Gram-positive aerobes[4].
Alatrofloxacin, the parenteral prodrug of Trovafloxacin, is a fluoronaphthyridone which contains an L-alanyl-L-alanyl salt. Alatrofloxacin functions similar to other fluoroquinolone antibiotics in that it not only has antibiotic activity to kill invading organisms by interfering with DNA synthesis, it possesses immunosuppressive activity[1].
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent[1][2][3][4].
DHODH-IN-7 is a human dihydroorotate dehydrogenase (DHODH) inhibitor, with an IC50 of 0.91 μM. DHODH-IN-7 induces differentiation in acute myeloid leukemia[1].
m7GpppAmpG is a trinucleotide cap analog with the capping efficiencies for the obtained RNAs of 90%[1].
Guanine-13C,15N2 is the 13C and 15N labeled Guanine[1]. Guanine (2-Aminohypoxanthine) is one of the fundamental components of nucleic acids (DNA and RNA). Guanine is a purine derivative, consisting of a fused pyrimidine-imidazole ring system with conjugated double bonds.
DMT-dG(ib) Phosphoramidite is typically used in the synthesis of DNA[1].
CX-5416 HCl is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
Di-tert-butyl diisopropylphosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.