Thymidylate Synthase
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.
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Thymidylate Synthase Related Products (74)
Related Products (74)
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Antibodies (1)
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MtTMPK-IN-5
0 ImagesCat. No.: HY-146699CAS No.: 2987763-18-6MtTMPK-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.
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TS-IN-6
0 ImagesCat. No.: HY-172172TS-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.
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TS-IN-2
0 ImagesCat. No.: HY-149849CAS No.: 2945983-00-4TS-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.
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ICI 198583
0 ImagesCat. No.: HY-113798CAS No.: 112887-62-4ICI 198583 is a thymidylate synthase (TS) inhibitor with a Ki value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia.
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Idetrexed
0 ImagesCat. No.: HY-10822CAS No.: 501332-69-0Synonyms: BGC 945; ONX-0801; CB 300945Idetrexed (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.
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CB 3705
0 ImagesCB 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.
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JMF4073
0 ImagesCat. No.: HY-162698CAS No.: 1927930-61-7JMF4073 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.
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CB3731
0 ImagesCat. No.: HY-123259CAS No.: 80015-07-2CB3731 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.
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LC1236
0 ImagesCat. No.: HY-184154CAS No.: 2756347-47-2LC1236 is a thymidylate synthase (hTS) dimer dissociator with a target Kd of 7 μM and poor transmembrane permeability. LC1236 inhibits enzymatic activity by shifting the monomer-dimer equilibrium toward inactive monomers. LC1236 acts as a cytotoxic agent to inhibit cancer cell growth, and exerts synergistic cytotoxicity with electroporation via enhancing intracellular accumulation. LC1236 can be used in the research of cancers such as ovarian cancer and colorectal cancer.
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2-Deoxyuridine-1,2,3,4,5-13C5
0 ImagesCat. No.: HY-W778990CAS No.: 478510-94-02-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).
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Trifluridine-13C,15N2
0 ImagesCat. No.: HY-A0061SCAS No.: 2086328-10-9Synonyms: Trifluorothymidine-13C,15N2; 5-Trifluorothymidine-13C,15N2; TFT-13C,15N2Trifluridine-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.
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MtTMPK-IN-2
0 ImagesCat. No.: HY-144664CAS No.: 2799607-71-7MtTMPK-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.
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CB 3717
0 ImagesCat. No.: HY-16638CAS No.: 76849-19-9Synonyms: PDDFCB 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.
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MtTMPK-IN-1
0 ImagesCat. No.: HY-144663CAS No.: 2799607-58-0MtTMPK-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.
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Galocitabine
0 ImagesCat. No.: HY-105262CAS No.: 124012-42-6Synonyms: Ro 09-1390Galocitabine (Ro 09-1390) is a nucleoside analog with anticancer and antiviral activity.
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EGFR/HER2/TS-IN-2
0 ImagesCat. No.: HY-146239CAS No.: 2444364-04-7EGFR/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.
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Idetrexed trisodium
0 ImagesCat. No.: HY-10822ACAS No.: 1097638-00-0Synonyms: BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodiumIdetrexed (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.
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LC1343
0 ImagesCat. No.: HY-184155CAS No.: 2756347-51-8LC1343 is a human thymidylate synthase (hTS) inhibitor with an IC50 of 7 μM. LC1343 inhibits cancer cell growth and induces apoptosis in cancer cells. LC1343 can be used for the research of ovarian cancer, colorectal cancer, and pancreatic cancer.
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MtTMPK-IN-8
0 ImagesCat. No.: HY-146702CAS No.: 2990619-92-4MtTMPK-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.
