2. Signaling Pathways
  3. Apoptosis
  4. Thymidylate Synthase

Thymidylate Synthase

Thymidylate Synthase

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture
    		Inhibitor 99.98%
    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.
    Trifluridine/tipiracil hydrochloride mixture
  • HY-10821
    Raltitrexed
    		Inhibitor 99.51%
    Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase.
    Raltitrexed
  • HY-A0061
    Trifluridine
    		Inhibitor 99.98%
    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.
    Trifluridine
  • HY-A0063A
    Tipiracil
    		Inhibitor 99.98%
    Tipiracil is a thymidine phosphorylase (TPase) inhibitor.
    Tipiracil
  • HY-D0186
    2'-Deoxyuridine
    		Inhibitor 99.98%
    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).
    2'-Deoxyuridine
  • HY-77537
    7-Deazaxanthine
    		99.72%
    7-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.
    7-Deazaxanthine
  • HY-172172
    TS-IN-6
    		Inhibitor
    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.
    TS-IN-6
  • HY-170648
    TS-IN-5
    		Inhibitor
    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.
    TS-IN-5
  • HY-103363
    SB-328437
    		Inhibitor 99.54%
    SB-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.
    SB-328437
  • HY-B0021
    Doxifluridine
    		Inhibitor 99.91%
    Doxifluridine 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.
    Doxifluridine
  • HY-109115
    Fosifloxuridine nafalbenamide
    		Inhibitor
    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.
    Fosifloxuridine nafalbenamide
  • HY-108474
    Nolatrexed dihydrochloride
    		Inhibitor 98.38%
    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.
    Nolatrexed dihydrochloride
  • HY-13728
    Plevitrexed
    		Inhibitor 98.00%
    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.
    Plevitrexed
  • HY-143207
    10-Formyl-5,8-dideazafolic acid
    		Inhibitor
    10-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor.
    10-Formyl-5,8-dideazafolic acid
  • HY-16110
    Tegafur-Uracil
    		Inhibitor 99.77%
    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.
    Tegafur-Uracil
  • HY-106168
    Thymectacin
    		98.21%
    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).
    Thymectacin
  • HY-D0186R
    2'-Deoxyuridine (Standard)
    		Inhibitor
    2'-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.
    2'-Deoxyuridine (Standard)
  • HY-10822
    Idetrexed
    		Inhibitor
    Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L.
    Idetrexed
  • HY-146699
    MtTMPK-IN-5
    		Inhibitor
    MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis.
    MtTMPK-IN-5
  • HY-149849
    TS-IN-2
    		Inhibitor
    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.
    TS-IN-2
Cat. No. Product Name / Synonyms Application Reactivity