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-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-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-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-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
  • 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-10822
    Idetrexed
    		Inhibitor
    Idetrexed (ONX 0801) is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer.
    Idetrexed
  • HY-122045
    CB 3705
    		Inhibitor
    CB 3705 is a dihydrofolate reductase (DHFR) and thymidylate synthetase (TS) inhibitor. CB 3705 inhibits L1210 cells and mutant L1210 cell line (L1210:C15) with ID50s of 4.77 μM and 408 μM, respectively.
    CB 3705
  • HY-162698
    JMF4073
    		Inhibitor
    JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC50s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo.
    JMF4073
  • HY-123259
    CB3731
    CB3731 is an analogue of N-10-(fluoroethyl)quinazolinylfolate and can be used for fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase.
    CB3731
  • HY-W778990
    2-Deoxyuridine-1,2,3,4,5-13C5
    2-Deoxyuridine-1,2,3,4,5-13C5 is the 13C-labeled 2'-Deoxyuridine (HY-D0186). 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-1,2,3,4,5-<sup>13</sup>C<sub>5</sub>
  • HY-A0061S
    Trifluridine-13C,15N2
    Trifluridine-13C,15N2 is the 13C and 15N labeled Trifluridine. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity.
    Trifluridine-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • HY-144664
    MtTMPK-IN-2
    		Inhibitor
    MtTMPK-IN-2 (compound 15) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 1.1 μM. MtTMPK-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-2 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 6.1 μM). MtTMPK-IN-2 can be used for researching tuberculosis.
    MtTMPK-IN-2
  • HY-16638
    CB 3717
    		Inhibitor
    CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10(-8) M). In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells.
    CB 3717
  • HY-144663
    MtTMPK-IN-1
    		Inhibitor
    MtTMPK-IN-1 (compound 3) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 2.5 μM. MtTMPK-IN-1 has moderate to weak activity against Mtb H37Rv and low cytotoxicity in human fibroblast cells MRC-5. MtTMPK-IN-1 can be used for researching tuberculosis.
    MtTMPK-IN-1
  • HY-105262
    Galocitabine
    		Inhibitor
    Galocitabine (Ro 09-1390) is a nucleoside analog with anticancer and antiviral activity.
    Galocitabine
  • HY-W142014
    N,O-Didansyl-L-tyrosine cyclohexylammonium
    		Inhibitor
    N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor, acts on TS of Escherichia coli, Lactobacillus casei and human with the IC50 values of 5.0, 3.4 and 119 μM, respectively.
    N,O-Didansyl-L-tyrosine cyclohexylammonium
  • 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
    Idetrexed trisodium
    		Inhibitor
    Idetrexed (ONX 0801) trisodium is a thymidylate synthase (TS) inhibitor with a Ki of 1.2 nM. Idetrexed trisodium can be specifically transported into α-folate receptor (α-FR)-overexpressing tumors, such as ovarian cancer.
    Idetrexed 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
Cat. No. Product Name / Synonyms Application Reactivity