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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Anticancer agent 315
0 ImagesCat. No.: HY-183108Anticancer agent 315 is an antitumor agent. Anticancer agent 315 binds to the active pocket of thymidylate synthase via forming strong hydrogen bonds with Lys487 and Ala498, stabilizing the arrangement of the ligand within the pocket. Anticancer agent 315 inhibits the proliferation of tumor cells. Anticancer agent 315 can be used for the research of liver cancer and breast cancer.
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TS-IN-8
0 ImagesCat. No.: HY-178911TS-IN-8 is a potent thymidylate synthase (TS) inhibitor. TS-IN-8 can induce apoptosis and cause cell cycle arrest at the G2/M in MCF-7 cells. TS-IN-8 can induce nuclear morphological changes. TS-IN-8 can increase intracellular reactive oxygen species (ROS) levels. TS-IN-8 can activate intrinsic apoptosis pathways by regulating apoptosis-related proteins such as the bax/bcl-2 ratio and caspase activation. TS-IN-8 can be used for the study of breast cancer.
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Vanoxonin
0 ImagesCat. No.: HY-122795CAS No.: 86933-99-5Vanoxonin is an inhibitor of thymidylate synthase found in Saccharopolyspora hirsuta with an IC50 value of 0.7 μg/mL.
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Folitixorin calcium
0 ImagesCat. No.: HY-14769ACAS No.: 133978-75-3Synonyms: 5,10-Methylenetetrafolate calcium; ANX-510Folitixorin calcium (5,10-Methylenetetrafolate calcium; ANX-510) is a reduced form of Folic acid (HY-16637) and a cofactor of thymidylate synthase. Folitixorin calcium acts as an essential cofactor to promote the formation of a tight ternary complex between thymidylate synthase and FdUMP, thereby enhancing the inhibitory effect of FdUMP on thymidylate synthase. Folitixorin calcium in combination with 5-fluorouracil and αVEGF reduces tumor volume in colorectal tumor models of nude mice. Folitixorin calcium is used in related research on Yoshida sarcoma, P-388 leukemia, and colorectal cancer.
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MtTMPK-IN-7
0 ImagesCat. No.: HY-146701CAS No.: 2987482-25-5MtTMPK-IN-7 (compound 26) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 47 μM. MtTMPK-IN-7 has sub-micromolar activity against mycobacteria (MICs = 2.3~4.7 μM) without significant cytotoxicity. MtTMPK-IN-7 can be used for researching tuberculosis.
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(Rac)-Plevitrexed
0 ImagesCat. No.: HY-13728BCAS No.: 153538-08-0Synonyms: (Rac)-ZD 9331; (Rac)-BGC9331(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Doxifluridine-d3
0 ImagesCat. No.: HY-B0021S1Synonyms: Ro 21-9738-d3; 5-Fluoro-5'-deoxyuridine-d3; 5'-DFUR-d3Doxifluridine-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.
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Metesind glucuronate
0 ImagesCat. No.: HY-19157CAS No.: 157182-23-5Synonyms: AG 331Metesind glucuronate (AG 331) is an inhibitor for thymidylate synthase with Ki of 1.2 nM. Metesind glucuronate inhibits the DNA synthesis and thus inhibits the cell viability of cancer cells with IC50 of 0.4-0.9 μM.
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Manninotriose (Standard)
0 ImagesCat. No.: HY-N0913RCAS No.: 13382-86-0Wy-45494 (hydrochloride) (Standard) is the analytical standard of Wy-45494 (hydrochloride). This product is intended for research and analytical applications. Wy-45494 hydrochloride (N-Desmethyl Venlafaxine hydrochloride; Wy 45494) is a minor active metabolite of the selective norepinephrine and serotonin reuptake inhibitor (SNRI) venlafaxine. It is formed from venlafaxine via the cytochrome P450 (CYP) isomer CYP3A4.2. Wy-45494 hydrochloride inhibits norepinephrine and serotonin reuptake in rat synaptosomal preparations (IC50s of 4.7 and 1.6 μM, respectively). In vivo, Wy-45494 hydrochloride reversed reserpine-induced hypothermia in mice at a minimum effective dose (MED) of 10 mg/kg.
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MtTMPK-IN-3
0 ImagesCat. No.: HY-144665CAS No.: 2799607-80-8MtTMPK-IN-3 (compound 25) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 0.12 μM. MtTMPK-IN-3 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis.
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EGFR/HER2/TS-IN-1
0 ImagesCat. No.: HY-146238CAS No.: 2444363-11-3EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis.
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MtTMPK-IN-9
0 ImagesCat. No.: HY-146703CAS No.: 2987299-68-1MtTMPK-IN-9 (compound 28) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 48 μM. MtTMPK-IN-9 has sub-micromolar activity against mycobacteria (MICs = 6.25~9.4 μM) without significant cytotoxicity. MtTMPK-IN-9 can be used for researching tuberculosis.
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Chlorasquin
0 ImagesCat. No.: HY-121256CAS No.: 18921-73-8Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.
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DG1
0 ImagesCat. No.: HY-149352DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model.
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Prokaryotic Thymidylate kinase
0 ImagesCat. No.: HY-E70912Prokaryotic thymidylate kinase (EC 2.7.4.9) is an enzyme that transfers phosphorus-containing groups (phosphotransferases) using phosphate groups as acceptors. Prokaryotic thymidylate kinase participates in pyrimidine metabolism. Its two substrates are ATP and dTMP, and its two products are ADP and dTDP.
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Doxifluridine (Standard)
0 ImagesSynonyms: Ro 21-9738 (Standard); 5-Fluoro-5'-deoxyuridine (Standard); 5'-DFUR (Standard)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.
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MAHS-3
0 ImagesCat. No.: HY-187513MAHS-3 is a thymidylate synthase (TS) and dihydrofolate reductase (DHFR) inhibitor, with IC50 values of 5.279 μM and 52.60 μM against human targets, respectively. MAHS-3 exhibits broad-spectrum antiproliferative activity against cancer cells, induces cell cycle arrest, activates endogenous caspase-dependent apoptosis, reduces MMP levels, inhibits cell migration, increases intracellular NO levels, and promotes autophagy activity. MAHS-3 can be used in cancer-related research.
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OSI-7904L
0 ImagesCat. No.: HY-10823CAS No.: 139987-54-5Synonyms: GW1843; 1843U89; OSI-7904OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a Ki of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma.
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MtTMPK-IN-6
0 ImagesCat. No.: HY-146700CAS No.: 2225885-99-2MtTMPK-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.
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MAHS-4
0 ImagesCat. No.: HY-187514MAHS-4 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR), with IC50 values of 1.918 μM and 83.53 μM, respectively. MAHS-4 inhibits thymidylate biosynthesis, reduces tetrahydrofolate pool maintenance, and interferes with extracellular matrix remodeling. MAHS-4 induces G2/M phase cell cycle arrest, activates endogenous caspase-dependent apoptosis, decreases MMP protein levels, inhibits cell migration, increases intracellular NO levels, and promotes autophagy activity. MAHS-4 is applicable for cancer-related research.
