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-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-W016819R
    5-Fluoroorotic acid (Standard)
    		Inhibitor
    5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity.
    5-Fluoroorotic acid (Standard)
  • 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
  • HY-103363R
    SB-328437 (Standard)
    		Inhibitor
    SB-328437 (Standard) is the analytical standard of SB-328437 (HY-103363). This product is intended for research and analytical applications. 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 (Standard)
  • HY-178288
    TS-IN-7
    		Inhibitor
    TS-IN-7 (Compound 6) is a thymidylate synthase (TS) inhibitor with an IC50 of 39 nM. TS-IN-7 can be used for the study of cancer chemotherapy.
    TS-IN-7
Cat. No. Product Name / Synonyms Application Reactivity