Thymidylate Synthase
Thymidylate synthase (TSase) is a key enzyme in cell proliferation as it catalyzes a reaction essential for DNA replication, a reductive methylation of 2′-deoxyuridine-5′-monophosphate (dUMP) to form 2′-deoxythymidine-5′-monophosphate (dTMP) using the co-substrate N5,N10-methylene-5,6,7,8-tetrahydrofolate (CH2H4F).
The activity and expression of TSase are tightly controlled throughout the cell cycle, particularly at the translational level. The TSase protein itself binds to the TSase mRNA both at the translational start site (TSS) and in the coding region, inhibiting translational processing of the message. TSase can also bind to the mRNA of at least nine other important gene products, including those of p53 and c-myc. Therefore, manipulating the level of the TSase protein could induce a cascade of consequential effects on cell growth. Because of its importance in DNA precursor synthesis and repair, TSase has proved to be an important target for many chemotherapeutic and antibiotic drugs. Structural analogs of dUMP (e.g., fluoropyrimidines) and CH2H4F (e.g., antifolates) are well-established drugs targeting thymidylate synthase.
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Thymidylate Synthase Related Products (69)
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Antibodies (1)
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Raltitrexed
0 ImagesSynonyms: ZD1694; D1694; ICI-D1694Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase.
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Trifluridine/tipiracil hydrochloride mixture
0 ImagesSynonyms: TAS-102; FTD/TPITrifluridine/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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Trifluridine
0 ImagesSynonyms: Trifluorothymidine; 5-Trifluorothymidine; TFTTrifluridine (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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SB-328437
0 ImagesSB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM. SB-328437 can inhibit eosinophil migration induced by eotaxin, eotaxin-2, and monocyte chemotactic protein-4. In addition, SB-328437 can sensitize 5-FU (HY-90006)-resistant gastric cancer cells. SB-328437 can also reduce the recruitment of neutrophils to the lungs and pulmonary inflammation during acute inflammation. SB-328437 can be used in the research of inflammation-related diseases.
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2'-Deoxyuridine
0 Images2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD).
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ICI 198583
0 ImagesCat. No.: HY-113798CAS No.: 112887-62-4ICI 198583 is a thymidylate synthase (TS) inhibitor with a Ki value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia.
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LC1236
0 ImagesCat. No.: HY-184154CAS No.: 2756347-47-2LC1236 is a thymidylate synthase (hTS) dimer dissociator with a target Kd of 7 μM and poor transmembrane permeability. LC1236 inhibits enzymatic activity by shifting the monomer-dimer equilibrium toward inactive monomers. LC1236 acts as a cytotoxic agent to inhibit cancer cell growth, and exerts synergistic cytotoxicity with electroporation via enhancing intracellular accumulation. LC1236 can be used in the research of cancers such as ovarian cancer and colorectal cancer.
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LC1343
0 ImagesCat. No.: HY-184155CAS No.: 2756347-51-8
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Tipiracil
0 ImagesTipiracil is a thymidine phosphorylase (TPase) inhibitor.
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5-Fluoroorotic acid monohydrate
0 ImagesSynonyms: 5-Fluorouracil-6-carboxylic acid Monohydrate; 5-FOA; 5-fluoro OA5-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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5-Fluoroorotic acid
0 Images5-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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Manninotriose
0 ImagesManninotriose is a natural functional trisaccharide composed of three mannose molecules. Manninotriose binds to dihydrofolate reductase via hydrogen bond formation with Arg28. Manninotriose binds to thymidylate synthase via hydrogen bond formation with Arg50. Manninotriose acts as a membrane protectant and helps improve stress tolerance. Manninotriose can be used in research related to acute lymphoblastic leukemia.
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Doxifluridine
0 ImagesSynonyms: Ro 21-9738; 5-Fluoro-5'-deoxyuridine; 5'-DFURDoxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs.
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7-Deazaxanthine
0 ImagesSynonyms: 7DX7-Deazaxanthine (7DX) is an inhibitor of thymidine phosphorylase (TPase). 7-Deazaxanthine inhibits TPase reaction in a concentration-dependent manner with an IC50 value of 40 μM. 7-Deazaxanthine also has a significant angiogenesis inhibitory effect.
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Fosifloxuridine nafalbenamide
0 ImagesCat. No.: HY-109115CAS No.: 1332837-31-6Synonyms: NUC-3373Fosifloxuridine 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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Plevitrexed
0 ImagesSynonyms: ZD 9331; BGC9331Plevitrexed (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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Nolatrexed dihydrochloride
0 ImagesSynonyms: AG 337Nolatrexed 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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FdUMP triethylammonium
0 ImagesSynonyms: 2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammoniumFdUMP 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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10-Formyl-5,8-dideazafolic acid
0 ImagesCat. No.: HY-143207CAS No.: 61038-31-110-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor.
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2'-Deoxyuridine (Standard)
0 Images2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD). In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine.
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min.
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain. 2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model.
