Search Result
Results for "
Thymidylate Synthase
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W011142
-
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dUMP disodium
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Endogenous Metabolite
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Infection
Metabolic Disease
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2'-Deoxyuridine 5'-monophosphate (dUMP) disodium is a deoxynucleotide that is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis .
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- HY-16110
-
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UFT; BMS-200604
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Thymidylate Synthase
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Cancer
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Tegafur-Uracil (UFT; BMS-200604) is an effective oral chemotherapy drug based on fluoropyrimidine. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used in combination with leucovorin (LV) and polysaccharide K (PSK) for research on solid tumors .
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- HY-16478
-
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TAS-102; FTD/TPI
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Nucleoside Antimetabolite/Analog
Thymidylate Synthase
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Cancer
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Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA .
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- HY-122795
-
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Thymidylate Synthase
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Others
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Vanoxonin is an inhibitor of thymidylate synthase found in Saccharopolyspora hirsuta with an IC50 value of 0.7 μg/mL .
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-
-
- HY-W394006
-
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dUMP
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Endogenous Metabolite
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Infection
Metabolic Disease
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2'-Deoxyuridine 5'-monophosphate (dUMP) is a deoxynucleotide that is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis .
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- HY-13728B
-
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(Rac)-ZD 9331; (Rac)-BGC9331
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Thymidylate Synthase
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Cancer
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(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-149849
-
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Thymidylate Synthase
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Cancer
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TS-IN-2 (compound 17) is a thymidylate synthase (TS) inhibitor with an IC50 of 0.81 μM. TS-IN-2 induces cancer cell apoptosis and cell cycle arrest in S phase, and also inhibit DNA synthesis, resulting in DNA damage .
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-
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- HY-13728A
-
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(R)-ZD 9331; (R)-BGC9331
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Biochemical Assay Reagents
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Cancer
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(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-W142014
-
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Thymidylate Synthase
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Cancer
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N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor, acts on TS of Escherichia coli, Lactobacillus casei and human with the IC50 values of 5.0, 3.4 and 119 μM, respectively .
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- HY-146239
-
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EGFR
Thymidylate Synthase
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Cancer
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EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
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-
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- HY-10821
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-
-
- HY-143207
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-
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- HY-108474
-
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AG 337
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Thymidylate Synthase
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Cancer
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Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.
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- HY-154508
-
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2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammonium
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Nucleoside Antimetabolite/Analog
Thymidylate Synthase
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Cancer
|
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FdUMP triethylammonium is the intracellular active form of 5-fluorouracil (5-FU). 5-FU is converted to FdUMP after being transported into the cell by various enzymes. FdUMP forms a ternary complex with thymidylate synthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylate synthase, which in turn leads to the suppression of DNA synthesis.
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- HY-162155
-
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Parasite
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Infection
|
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Diarctigenin is a selective Leishmania major dihydrofolate reductase-thymidylate synthase (LmDHFR-TS) inhibitor. Diarctigenin can be used for the research of tropical disease .
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- HY-117247
-
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DNA/RNA Synthesis
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Infection
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5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor with inhibitory activity against other folate-related enzymes. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed mild growth inhibition against enterococci, lactic acid bacteria, and L1210 cells in culture. 5,6,7,8-Tetrahydro-8-deazahomofolic acid also showed weak inhibition against thymidylate synthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylate synthase .
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- HY-10821R
-
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Thymidylate Synthase
Nucleoside Antimetabolite/Analog
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Cancer
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Raltitrexed (Standard) is the analytical standard of Raltitrexed. This product is intended for research and analytical applications. Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase.
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- HY-W076898A
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Antibiotic
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Others
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Hydroxyethyl disulfide blocks the inhibitory effect of showdomycin on methotrexate-resistant thymidylate synthase and is also protected by its substrate deoxyuridylic acid, preventing inactivation of the antibiotic .
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- HY-W016819
-
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Thymidylate Synthase
Parasite
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Infection
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5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity .
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- HY-118251
-
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Antifolate
Dihydrofolate reductase (DHFR)
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Cancer
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PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
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- HY-W016819R
-
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Thymidylate Synthase
Parasite
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Infection
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5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity .
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- HY-N14161
-
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Thymidylate Synthase
Apoptosis
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Cancer
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Diazaquinomycin A (DAQA), a diaza-anthracene antibiotic, is a thymidylate synthase inhibitor. Diazaquinomycin A (DAQA) induces DNA damage, cell cycle arrest, and apoptosis through cleaved-PARP .
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- HY-120293
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Thymidylate Synthase
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Cancer
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CB30900 is an inhibitor for thymidylate synthase with an IC50 of 0.2 μM. CB30900 exhibits cytotoxicity in W1L2 with an IC50 of 0.13 μM .
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- HY-106168
-
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NB1011
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Thymidylate Synthase
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Cancer
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Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin) .
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- HY-123259
-
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Thymidylate Synthase
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Others
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CB3731 is an analogue of N-10-(fluoroethyl)quinazolinylfolate and can be used for fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase .
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-
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- HY-10820B
-
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LY231514 disodium heptahydrate
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Antifolate
Autophagy
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Cancer
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Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
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- HY-13781
-
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LY231514 disodium hemipenta hydrate
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Antifolate
Autophagy
Apoptosis
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Cancer
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Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
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- HY-10820
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Pemetrexed
Maximum Cited Publications
35 Publications Verification
LY231514
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Antifolate
Autophagy
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Cancer
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Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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-
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- HY-10822
-
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BGC 945; ONX-0801; CB 300945
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Thymidylate Synthase
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Cancer
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Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .
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- HY-10820A
-
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LY231514 disodium
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Antifolate
Autophagy
Apoptosis
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Cancer
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Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-19157
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AG 331
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Thymidylate Synthase
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Cancer
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Metesind glucuronate (AG 331) is an inhibitor for thymidylate synthase with Ki of 1.2 nM. Metesind glucuronate inhibits the DNA synthesis and thus inhibits the cell viability of cancer cells with IC50 of 0.4-0.9 μM .
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- HY-10822A
-
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BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodium
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Thymidylate Synthase
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Cancer
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Idetrexed (ONX 0801) trisodium is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed trisodium can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .
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- HY-109115
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NUC-3373
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Thymidylate Synthase
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Cancer
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Fosifloxuridine nafalbenamide (NUC-3373), a pyrimidine nucleotide analogue, is a Thymidylate synthase inhibitor. Fosifloxuridine nafalbenamide has anticancer activity. Fosifloxuridine nafalbenamide has the potential to evoke a host immune response and enhance immunoresearch .
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- HY-162698
-
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Thymidylate Synthase
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Cancer
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JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC50s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo .
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- HY-W016819B
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5-Fluorouracil-6-carboxylic acid Mono(hydrate); 5-FOA; 5-fluoro OA
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Thymidylate Synthase
Parasite
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Infection
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5-Fluoroorotic acid monohydrate is the monohydrate salt form of 5-Fluoroorotic acid (HY-W016819).
5-Fluoroorotic acid monohydrate is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid monohydrate exhibits antimalarial activity .
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- HY-10820S
-
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LY231514-d5
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Antifolate
Autophagy
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Cancer
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Pemetrexed-d5 is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-10820R
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LY231514 (Standard)
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Reference Standards
Antifolate
Autophagy
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Cancer
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Pemetrexed (Standard) is the analytical standard of Pemetrexed. This product is intended for research and analytical applications. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-10820AS
-
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LY231514-dd5 disodium
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Isotope-Labeled Compounds
Antifolate
Autophagy
Apoptosis
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Cancer
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Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-10823
-
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GW1843; 1843U89; OSI-7904
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Antifolate
Thymidylate Synthase
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Cancer
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OSI-7904L (GW1843) is a noncompetitive inhibitor of thymidylate synthase (TS). OSI-7904L is an antifolate compound and a substrate for folylpolyglutamate synthetase. OSI-7904L has cytotoxicity against solid tumor lines, and the toxicity can be selectively blocked by folic acid .
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- HY-170648
-
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Thymidylate Synthase
Apoptosis
PI3K
STAT
Bcl-2 Family
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Cancer
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TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers .
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- HY-10820BR
-
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LY231514 disodium heptahydrate (Standard)
|
Reference Standards
Antifolate
Autophagy
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Cancer
|
|
Pemetrexed (disodium heptahydrate) (Standard) is the analytical standard of Pemetrexed (disodium heptahydrate). This product is intended for research and analytical applications. Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
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- HY-13781R
-
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Antifolate
Autophagy
Apoptosis
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Cancer
|
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Pemetrexed (disodium hemipenta hydrate) (Standard) is the analytical standard of Pemetrexed (disodium hemipenta hydrate). This product is intended for research and analytical applications. Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
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- HY-168918
-
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Parasite
Dihydrofolate reductase (DHFR)
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Infection
|
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Insecticidal agent 19 (Compound 7b) exhibits antimalarial activity by inhibiting dihydrofolate
reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) through the folic acid metabolic pathway. Insecticidal agent 19 inhibits Leishmania major promastigote and amastigote with IC50 of 1.43 μM and 3.78 μM .
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- HY-A0061
-
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Trifluorothymidine; 5-Trifluorothymidine; TFT
|
Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
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Cancer
|
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Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
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-
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- HY-14520A
-
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(6S)-5,6,7,8-Tetrahydrofolic acid
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Endogenous Metabolite
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Metabolic Disease
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(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .
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-
-
- HY-A0061S
-
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Trifluorothymidine-13C,15N2; 5-Trifluorothymidine-13C,15N2; TFT-13C,15N2
|
Thymidylate Synthase
Nucleoside Antimetabolite/Analog
HSV
Orthopoxvirus
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Cancer
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Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine . Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity .
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-
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- HY-149352
-
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Thymidylate Synthase
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Cancer
|
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
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-
- HY-172172
-
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Thymidylate Synthase
Apoptosis
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Cancer
|
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TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, demonstrating significant antiproliferative activity. TS-IN-6 induces G1 phase cell cycle arrest and apoptosis (marked by substantial increases in both early and late apoptotic rates) and shows potential for research on cancers such as colon, breast, and liver cancers .
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-
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- HY-W769288
-
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LY231514 disodium-13C5
|
Isotope-Labeled Compounds
Apoptosis
Antifolate
Autophagy
|
Cancer
|
|
Pemetrexed disodium- 13C5 (LY231514 disodium- 13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-146238
-
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EGFR
Thymidylate Synthase
Apoptosis
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Cancer
|
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EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .
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-
- HY-A0061R
-
|
Trifluorothymidine (Standard); 5-Trifluorothymidine (Standard); TFT (Standard)
|
Reference Standards
Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
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Cancer
|
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Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
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- HY-13728
-
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ZD 9331; BGC9331
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Thymidylate Synthase
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Cancer
|
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Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical . Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-124093
-
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Thymidylate Synthase
Bacterial
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Infection
Cancer
|
8-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitory activity against folate-dependent S. faecium, L. casei, and MTX (HY-14519) resistant strains. 8-Deazahomofolic acid also inhibits the growth of L1210 leukemia cells, with an IC50 value of 87.5 μM. 8-Deazahomofolic acid can be used in research on bacterial infections and tumors .
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-
- HY-116217
-
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FdCyd; NSC-48006
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DNA Methyltransferase
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Cancer
|
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5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity .
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- HY-116217R
-
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DNA Methyltransferase
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Cancer
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5-Fluoro-2'-deoxycytidine (Standard) is the analytical standard of 5-Fluoro-2'-deoxycytidine. This product is intended for research and analytical applications. 5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity .
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-
- HY-134160
-
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5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil
|
Nucleoside Antimetabolite/Analog
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Cancer
|
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5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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- HY-134160S
-
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5-DHFU-13C,15N2; 5-Fluorodihydropyrimidine-2,4-dione-13C,15N2; 5-Fluorodihydrouracil-13C,15N2
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Isotope-Labeled Compounds
Nucleoside Antimetabolite/Analog
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Cancer
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5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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HY-L044
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593 compounds
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Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications.
MCE offers a unique collection of 593 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).
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Target |
Research Area |
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- HY-W142014
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Thymidylate Synthase
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Cancer
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N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor, acts on TS of Escherichia coli, Lactobacillus casei and human with the IC50 values of 5.0, 3.4 and 119 μM, respectively .
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Target |
Chemical Structure |
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Product Name |
Chemical Structure |
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- HY-10820S
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Pemetrexed-d5 is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-10820AS
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Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-A0061S
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Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine . Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity .
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- HY-W769288
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Pemetrexed disodium- 13C5 (LY231514 disodium- 13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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- HY-134160S
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5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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* This product has been "discontinued".
Optimized version of product available:
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Classification |
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- HY-13728
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ZD 9331; BGC9331
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Alkynes
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Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical . Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-13728B
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(Rac)-ZD 9331; (Rac)-BGC9331
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Alkynes
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(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-13728A
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(R)-ZD 9331; (R)-BGC9331
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Alkynes
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(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-120293
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Alkynes
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CB30900 is an inhibitor for thymidylate synthase with an IC50 of 0.2 μM. CB30900 exhibits cytotoxicity in W1L2 with an IC50 of 0.13 μM .
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- HY-10822
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BGC 945; ONX-0801; CB 300945
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Alkynes
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Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .
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- HY-10822A
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BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodium
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Alkynes
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Idetrexed (ONX 0801) trisodium is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed trisodium can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer .
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Product Name |
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Classification |
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- HY-W011142
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dUMP disodium
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Nucleotide Analogs
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2'-Deoxyuridine 5'-monophosphate (dUMP) disodium is a deoxynucleotide that is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis .
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- HY-154508
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2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammonium
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Nucleoside Analogs
Uridine
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FdUMP triethylammonium is the intracellular active form of 5-fluorouracil (5-FU). 5-FU is converted to FdUMP after being transported into the cell by various enzymes. FdUMP forms a ternary complex with thymidylate synthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylate synthase, which in turn leads to the suppression of DNA synthesis.
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- HY-W394006
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dUMP
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Nucleotide Analogs
Uracil Nucleotide
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2'-Deoxyuridine 5'-monophosphate (dUMP) is a deoxynucleotide that is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis .
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