1. Signaling Pathways
  2. Apoptosis
  3. Thymidylate Synthase

Thymidylate Synthase

Thymidylate synthase (TS) is an E2F1-regulated enzyme that is essential for DNA synthesis and repair. Thymidylate synthase is an essential S phase enzyme required for DNA synthesis. Thymidylate synthase plays a central role in the biosynthesis of thymidylate, an essential precursor for DNA synthesis.

Thymidylate synthase catalyzes the reductive methylation of 2′-deoxyuridine 5-monophosphate (dUMP) by transfer of a methylene group from a cofactor, CH2H4 folate, to generate deoxythymidine-5′-monophoshate (dTMP). dTMP is further phosphorylated to the triphosphate state (dTTP), which is a direct precursor for DNA synthesis. Since the TS catalyzed reaction is the sole intracellular de novo source of dTMP, the inhibition of TS results in the cessation of cellular proliferation and growth.

Thymidylate synthase protein and mRNA levels are elevated in many human cancers, and high TS levels have been correlated with poor prognosis in patients with colorectal, breast, cervical, bladder, kidney, and non-small cell lung cancers.

Thymidylate Synthase Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-10821
    Raltitrexed Inhibitor ≥98.0%
    Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture Inhibitor ≥98.0%
    Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio.
  • HY-A0061
    Trifluridine Inhibitor 99.85%
    Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection.
  • HY-A0063A
    Tipiracil Inhibitor
    Tipiracil is a thymidine phosphorylase (TPase) inhibitor.
  • HY-108474
    Nolatrexed dihydrochloride Inhibitor 98.21%
    Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity.
  • HY-109115
    Fosifloxuridine nafalbenamide Inhibitor 98.18%
    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 immunotherapy.
  • HY-10822A
    ONX 0801 trisodium Inhibitor
    ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
  • 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.
  • HY-13728
    Plevitrexed Inhibitor
    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.
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