Nucleoside Antimetabolite/Analog

5-BrdU (Broxuridine) , a nucleoside analog, are used in the detection of proliferating cells and competes with thymidine for incorporation into DNA.

Sangivamycin (NSC-65346) is an effective inhibitor of protein kinase C (PKC, Ki = 10 μM). Sangivamycin exhibits antiproliferative activity against a variety of human cancers.

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

5-Azacytidine (Ladakamycin) is a cytidine nucleoside analog, a DNA methylation inhibitor with specificity. 5-Azacytidine regulates gene expression by decreasing the level of DNA methylation. 5-Azacytidine induces autophagy and has antitumor activity.

Trifluridine tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug containing trifluridine (TFT) and tipiracil hydrochloride (TTP) in a 2:1 molar ratio.

Peldesine (BCX 34) is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.

Ascamycin is a 5'-O-sulfonamide ribonucleoside antibiotic produced by Streptomyces spp. It exhibits selective antibacterial activity against Xanthomonas species, inhibiting Xanthomonas citri, Xanthomonas oryzae, and phage with MIC values of 0.4 μg mL, 12.5 μg mL, and 12.5 μg mL respectively.

Gemcitabine hydrochloride (LY 188011 hydrochloride) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.

Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.

Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.

5-Ethynyluridine is a clickable form of uridine.1It is incorporated into cellular RNA, but not DNA, and has been used to detect transcriptionin vitroandin vivo. 1.Jao, C.Y., and Salic, A.Exploring RNA transcription and turnover in vivo by using click chemistryProc. Natl. Acad. Sci. USA105(41)15779-15784(2008)

Adenosine (D-Adenosine) is a natural product, a ribonucleoside consisting of adenine bound to ribose. Adenosine has vasodilatory, antiarrhythmic and analgesic effects.

Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

Tipiracil hydrochloride (MA-1 hydrochloride) is a thymidine phosphorylase inhibitor (TPI). Tipiracil hydrochloride is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials.

Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.

N6-Methyl-2'-O-methyladenosine (N6,2′-O-Dimethyladenosine), a substrate for adiposity and obesity-related genes (FTO), is a reversible modifier compound found on a wide variety of RNA molecules.N6,2′-O-Dimethyladenosine can be used to study obesity and its related diseases.

Orotic acid (Vitamin B13) is an intermediate product in pyrimidine metabolism.

Uridine-5-acetic acid (5-Carboxymethyluridine) is a nucleoside formed during yeast and wheat embryo transfer RNA processes, which can be used for cell labeling and tracking DNA synthesis.

RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

Deoxycytidine triphosphate is a nucleoside triphosphate.It is a raw material in DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.

Trifluridine (NSC-75520) is a fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity.

Clofarabine (Clofarex)m, a second generation purine nucleoside analog with antineoplastic activity, inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

6-Mercaptopurine (6-MP) is an antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.

N,N-Dimethyl-2'-O-methylcytidine (N4,N4,2'-O-Trimethylcytidine) is a purine nucleoside analog with anticancer activity. It selectively inhibits DNA synthesis in cells, thereby suppressing cell growth.

Fludarabine Phosphate (NSC 312887 Phosphate) is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.

8-Azaguanine (SK 1150) is a purine analogue with potential antineoplastic activity.

Raltitrexed (D1694)(IC50 of 9 nM), a thymidylate synthase inhibitor, is used for the inhibition of L1210 cell growth.

Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy.

3-Methylcytidine as biomarkers of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer.

Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.

2-Thiocytidine is a purine nucleoside analog that targets malignant tumors of the inert lymphatic system and possesses a broad spectrum of antitumor activity. It induces apoptosis by inhibiting DNA synthesis.

N2-Methylguanosine is a modified nucleoside found at several specific sites in various tRNAs.

Isoguanine, a purine base and isomer of guanine, serves as a building block in organic synthesis.

dGTP (2'-Deoxyguanosine-5'-triphosphate) is a guanosine nucleotide highly susceptible to oxidative damage, resulting in 8-O-GDP, 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.

8-Chloroinosine is a purine nucleoside analog and a metabolite of the anticancer compound 8-chloro-adenosine.

N1-Methylpseudouridine-5'-triphosphate is a modified nucleotide derivative commonly used to explore RNA modification, synthesis, and function, and can replace UTP in synthesis thereby improving RNA stability and reducing immunogenicity.

2'-Deoxy-N4-methylcytidine (N(3)-Methyl-2'-deoxycytidine) is a purine nucleoside analog with potential antitumor activity for the study of apoptosis.

N6-(p-Methoxybenzyl)adenosine is an adenosine analog that shows in vitro antiproliferative activity in U87MG glioma cells and immunogenicity in isolated γδ T cells derived from stimulated peripheral blood mononuclear cells (PBMCs).

5'-Azido-5'-deoxythymidine is a nucleoside analog with potential anti-tuberculosis activity as an inhibitor of Mycobacterium tuberculosis monophosphate kinase (TMPKmt), an enzyme essential for DNA replication in Mycobacterium tuberculosis. 5'-Azido-5'-deoxythymidine contains an azide group in its molecular structure, which enhances its ability to inhibit reverse transcriptase, and is commonly used in the study of nucleoside metabolic pathways and related disease mechanisms.

1-Methylinosine (N1-Methylinosine) is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA and has a role as a metabolite.

DMTr-LNA-5MeU-3-CED-phosphoramidite, a nucleoside derivative, is a modified building block used in oligonucleotide synthesis to enhance stability and binding affinity.

2'-Deoxy-5,6-dihydrouridine is a nucleoside analog that contains a dihydro group in its molecular structure and is commonly used in base excision related studies.