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-146239
    EGFR/HER2/TS-IN-2
    		Inhibitor
    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.
    EGFR/HER2/TS-IN-2
  • HY-10822A
    ONX 0801 trisodium
    		Inhibitor
    ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
    ONX 0801 trisodium
  • HY-146702
    MtTMPK-IN-8
    		Inhibitor
    MtTMPK-IN-8 (compound 27) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor. MtTMPK-IN-8 has sub-micromolar activity against mycobacteria (MICs = 0.78~9.4 μM) without significant cytotoxicity. MtTMPK-IN-8 can be used for researching tuberculosis.
    MtTMPK-IN-8
  • HY-146701
    MtTMPK-IN-7
    		Inhibitor
    MtTMPK-IN-7 (compound 26) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 47 μM. MtTMPK-IN-7 has sub-micromolar activity against mycobacteria (MICs = 2.3~4.7 μM) without significant cytotoxicity. MtTMPK-IN-7 can be used for researching tuberculosis.
    MtTMPK-IN-7
  • HY-13728B
    (Rac)-Plevitrexed
    		Inhibitor
    (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.
    (Rac)-Plevitrexed
  • 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-19157
    Metesind glucuronate
    		Inhibitor
    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.
    Metesind glucuronate
  • HY-144665
    MtTMPK-IN-3
    		Inhibitor
    MtTMPK-IN-3 (compound 25) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 0.12 μM. MtTMPK-IN-3 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis.
    MtTMPK-IN-3
  • HY-146238
    EGFR/HER2/TS-IN-1
    		Inhibitor
    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.
    EGFR/HER2/TS-IN-1
  • HY-146703
    MtTMPK-IN-9
    		Inhibitor
    MtTMPK-IN-9 (compound 28) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 48 μM. MtTMPK-IN-9 has sub-micromolar activity against mycobacteria (MICs = 6.25~9.4 μM) without significant cytotoxicity. MtTMPK-IN-9 can be used for researching tuberculosis.
    MtTMPK-IN-9
  • HY-121256
    Chlorasquin
    		Inhibitor
    Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.
    Chlorasquin
  • HY-149352
    DG1
    		Inhibitor
    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.
    DG1
  • HY-B0021R
    Doxifluridine (Standard)
    		Inhibitor
    Doxifluridine (Standard) is the analytical standard of Doxifluridine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-146700
    MtTMPK-IN-6
    		Inhibitor
    MtTMPK-IN-6 (compound 1) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 29 μM. MtTMPK-IN-6 can be used for researching tuberculosis.
    MtTMPK-IN-6
  • HY-120293
    CB30900
    		Inhibitor
    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.
    CB30900
  • HY-124093
    8-Deazahomofolic acid
    		Inhibitor
    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.
    8-Deazahomofolic acid
  • HY-154508
    FdUMP triethylammonium
    		Inhibitor
    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.
    FdUMP triethylammonium
  • HY-A0061R
    Trifluridine (Standard)
    		Inhibitor
    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.
    Trifluridine (Standard)
  • HY-B0021S1
    Doxifluridine-d3
    		Inhibitor
    Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). 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-d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity