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-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-10823
    OSI-7904L
    		Inhibitor
    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.
    OSI-7904L
  • 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 99.96%
    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-W129441
    N-Acetyl-4-S-cysteaminylphenol
    		Inhibitor
    N-Acetyl-4-S-mercaptoaminophenol (N-Ac-4-S-CAP) is a compound that is selectively cytotoxic to melanocytes of black mouse hair follicles. It can cause 98% depigmentation of black mouse hair follicles. N-Ac-4-S-CAP can produce visible changes in hair follicle melanocytes 4 hours after intraperitoneal injection, including aggregation of melanin granules and nuclear condensation. Electron microscopy observations showed that it caused progressive destruction of melanocytes, including swelling of membranous organelles, nuclear condensation, and cytoplasmic vacuolation, ultimately leading to complete cell necrosis. N-Ac-4-S-CAP has a specific cytotoxic effect on melanocytes that actively produce eumelanin, but may not affect precursor or dormant melanocytes. These properties suggest that N-Ac-4-S-CAP may have potential application value in the treatment of melanoma or skin whitening.
    N-Acetyl-4-S-cysteaminylphenol
  • 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>
  • HY-N14161
    Diazaquinomycin A
    		Inhibitor
    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.
    Diazaquinomycin A
Cat. No. Product Name / Synonyms Application Reactivity