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Nucleoside Antimetabolite/Analog

Nucleoside analogues are molecules that act like nucleosides in DNA synthesis. They include a range of antiviral products used to prevent viral replication in infected cells. Nucleoside analogues can be used against hepatitis B virus, hepatitis C virus, herpes simplex, and HIV. Once they are phosphorylated, they work as antimetabolites by being similar enough to nucleotidesto be incorporated into growing DNA strands.

Gemcitabine
T025195058-81-4
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.
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Decitabine
T15082353-33-5
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.
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5-Fluorouracil
T098451-21-8
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.
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Fludarabine
T103821679-14-1
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.
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5-BrdU
T679459-14-3
5-BrdU (Broxuridine) , a nucleoside analog, are used in the detection of proliferating cells and competes with thymidine for incorporation into DNA.
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Gemcitabine hydrochloride
T6069122111-03-9
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.
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Tipiracil hydrochloride
T2366183204-72-0
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.
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2’-Deoxy-N4-methylcytidine
TNU120522882-02-6
2’-Deoxy-N4-methylcytidine (N(3)-Methyl-2'-deoxycytidine) is a purine nucleoside analog with potential antitumor activity for the study of apoptosis.
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Sangivamycin
T960518417-89-5
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.
  • $128
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Rabacfosadine
T16716859209-74-8In house
Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.
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LY2334737
T4061892128-60-8
LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity.
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Capecitabine
T1408154361-50-9
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.
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5-Ethynyluridine
T3697169075-42-9
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)
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Floxuridine
T096450-91-9
Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.
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Peldesine
T12399133432-71-0In house
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.
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RX-3117
T16813865838-26-2
RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.
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N2-Methylguanosine
T75142140-77-4
N2-Methylguanosine is a modified nucleoside found at several specific sites in various tRNAs.
  • $53
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CNDAC hydrochloride
T13621134665-72-8
CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.
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Ganciclovir
T068882410-32-0
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.
  • $51
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Clofarabine
T0297123318-82-1
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.
  • $36
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Trifluridine
T142870-00-8
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.
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Dacarbazine
T11204342-03-4
Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.
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Raltitrexed
T6632112887-68-0
Raltitrexed (D1694)(IC50 of 9 nM), a thymidylate synthase inhibitor, is used for the inhibition of L1210 cell growth.
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LNA-Adenosine
T32826206055-70-1
LNA-Adenosine (LNA-A) is a nucleoside analogue that acts as a ligand for adenosine A3 receptors.
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dGTP
T401922564-35-4
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.
  • $148
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3-Methylcytidine
T73512140-64-9
3-Methylcytidine as biomarkers of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer.
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6-Mercaptopurine
T001050-44-2
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.
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Fludarabine Phosphate
T650175607-67-9
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.
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2-Thiocytidine
TNU043613239-97-9
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.
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Carmofur
T130761422-45-5
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.
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Deoxyguanosine triphosphate trisodium salt
T3668893919-41-6
Deoxyguanosine triphosphate trisodium salt (2'-Deoxyguanosine-5'-triphosphate trisodium salt) is a nucleotide precursor for DNA synthesis in cells and can be used in the reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification.
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7-Methylxanthine
T0543552-62-5
7-Methylxanthine is a methyl derivative of xanthine, the purine component of human urinary calculi.7-Methylxanthine has an affinity for adenosine receptors.7-Methylxanthine is a methyl derivative of xanthine, the purine component of human urinary calculi.7-Methylxanthine has an affinity for adenosine receptors.
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Trifluridine/tipiracil hydrochloride mixture
T3658733030-01-8
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.
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1-Methylinosine
T190832140-73-0
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.
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N6-Methyl-2'-O-methyladenosine
TNU035557817-83-1
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.
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Deoxycytidine triphosphate
T75202056-98-6
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.
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6-​Thioinosine
T7621574-25-4
6-Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent.
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Isoguanine
T193823373-53-3
Isoguanine, a purine base and isomer of guanine, serves as a building block in organic synthesis.
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Deoxycytidine triphosphate trisodium salt
T7518109909-44-6
Deoxycytidine triphosphate trisodium salt (2'-DEOXYCYTIDINE-5'-TRIPHOSPHATE TRISODI) contributes to antibiotic lethality in stationary-phase mycobacteria.
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Nelarabine
T6603121032-29-9
Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
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1-Methylcytosine
T100191122-47-0In house
1-Methylcytosine (4-amino-1-methylpyrimidin-2(1H)-one) is a methylated form of the cytosine and can be used as the nucleobase of hachimoji DNA paired with isoguanine.
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Sapacitabine
TQ0245151823-14-2
Sapacitabine (CS682) is an orally available nucleoside analog precursor compound with potential anti-tumor activity for the study of acute myeloid leukemia.
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N6-Methyladenine
T36572443-72-1
N6-Methyladenine (6-(Methylamino)Purine) is a modified purine commonly found in genomes of prokaryotes, protists, and plants. N6-methyladenine affects diverse DNA functions, including replication, repair, and expression.
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8-Azahypoxanthine
T201022683-90-1
8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.
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N6,N6-Dimethyladenosine
T194642620-62-4
N6,N6-Dimethyladenosine is find in mycobacterium bovis Bacille Calmette-Guérin tRNA.
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5-Hydroxyuridine
TNU0031957-77-7
5-Hydroxyuridine (OHUrd) is a purine nucleoside analogue with potential antitumor activity, demonstrating cytotoxicity against human colon adenocarcinoma cell lines.
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Ara-G
T3694438819-10-2
Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).
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2’-OMe-Guanosine
T97262140-71-8
2'-OMe-Guanosine is a modified nucleoside produced by the action of tRNA guanosine-2'-o-methyltransferase. 2'-OMe-Guanosine has a certain pro-apoptotic effect.
  • $32
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