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2'-Deoxyuridine 5'-monophosphate disodium is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylatesynthase (TS). dTMP is a nucleotide required for DNA synthesis .
Tegafur-Uracil (UFT; BMS-200604) is an effective oral chemotherapy drug based on fluoropyrimidine. Tegafur-Uracil inhibits thymidylatesynthase. Tegafur-Uracil can be used in combination with leucovorin (LV) and polysaccharide K (PSK) for research on solid tumors .
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 thymidylatesynthase (TS) and incorporation into DNA .
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylatesynthase (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.
TS-IN-2 (compound 17) is a thymidylatesynthase (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 .
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylatesynthase (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.
N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylatesynthase (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 .
Idetrexed is a thymidylatesynthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylatesynthase with a Ki of 1.2 nmol/L .
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylatesynthase) 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 .
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylatesynthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylatesynthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
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 thymidylatesynthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylatesynthase, which in turn leads to the suppression of DNA synthesis.
Diarctigenin is a selective Leishmania major dihydrofolate reductase-thymidylatesynthase (LmDHFR-TS) inhibitor. Diarctigenin can be used for the research of tropical disease .
Hydroxyethyl disulfide blocks the inhibitory effect of showdomycin on methotrexate-resistant thymidylatesynthase and is also protected by its substrate deoxyuridylic acid, preventing inactivation of the antibiotic .
5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylatesynthase (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 thymidylatesynthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylatesynthase .
PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylatesynthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylatesynthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin) .
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 thymidylatesynthase .
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
Metesind glucuronate (AG 331) is an inhibitor for thymidylatesynthase 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 .
Fosifloxuridine nafalbenamide (NUC-3373), a pyrimidine nucleotide analogue, is a Thymidylatesynthase inhibitor. Fosifloxuridine nafalbenamide has anticancer activity. Fosifloxuridine nafalbenamide has the potential to evoke a host immune response and enhance immunoresearch .
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 .
Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of the potent thymidylatesynthase inhibitor 5-fluoro-2′-dUMP .
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].
TS-IN-5 (Compound 15) is a thymidylatesynthase (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 .
Pemetrexed (disodium) (Standard) is the analytical standard of Pemetrexed (disodium). This product is intended for research and analytical applications. 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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylatesynthase 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 .
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylatesynthase 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 .
Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine[1]. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylatesynthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity[2].
DG1 (Compound 8Nc) is a ThymidylateSynthase (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 .
EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylatesynthase) 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 .
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 thymidylatesynthase 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 .
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylatesynthase (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.
8-Deazahomofolic acid is an inhibitor of thymidylatesynthase (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 .
5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylatesynthase 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.
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 thymidylatesynthase. 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 548 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).
N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylatesynthase (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 .
2'-Deoxyuridine 5'-monophosphate disodium is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylatesynthase (TS). dTMP is a nucleotide required for DNA synthesis .
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylatesynthase 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 .
Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
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 thymidylatesynthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].
Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine[1]. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylatesynthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity[2].
Thymidylate Synthase Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 36 kDa, targeting to thymidylate synthase. It can be used for WB, IHC-F, IHC-P, ICC/IF, IP assays with tag free, in the background of Human.
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylatesynthase (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.
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylatesynthase (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.
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylatesynthase (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.
Idetrexed is a thymidylatesynthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylatesynthase with a Ki of 1.2 nmol/L .
2'-Deoxyuridine 5'-monophosphate disodium is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylatesynthase (TS). dTMP is a nucleotide required for DNA synthesis .
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 thymidylatesynthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylatesynthase, which in turn leads to the suppression of DNA synthesis.
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