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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2',2'-Difluorodeoxyuridine 5'-monophosphate
0 ImagesCat. No.: HY-185841CAS No.: 139729-89-8Synonyms: dFdUMP2',2'-Difluorodeoxyuridine 5'-monophosphate (dFdUMP) is a metabolite of Gemcitabine (HY-17026) and an inhibitor of Thymidylate synthase, with an inhibition constant of 130 μM. 2',2'-Difluorodeoxyuridine 5'-monophosphate can be used in research related to ovarian cancer, hematologic malignancies, non-small cell lung cancer, pancreatic cancer, soft tissue sarcoma, and glioblastoma multiforme.
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CB30900
0 ImagesCat. No.: HY-120293CAS No.: 145788-82-5CB30900 is an inhibitor for thymidylate synthase with an IC50 of 0.2 μM. CB30900 exhibits cytotoxicity in W1L2 with an IC50 of 0.13 μM.
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8-Deazahomofolic acid
0 ImagesCat. No.: HY-124093CAS No.: 111113-73-68-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitory activity against folate-dependent S. faecium, L. casei, and MTX (HY-14519) resistant strains. 8-Deazahomofolic acid also inhibits the growth of L1210 leukemia cells, with an IC50 value of 87.5 μM. 8-Deazahomofolic acid can be used in research on bacterial infections and tumors.
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Trifluridine (Standard)
0 ImagesSynonyms: Trifluorothymidine (Standard); 5-Trifluorothymidine (Standard); TFT (Standard)Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.
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Raltitrexed (Standard)
0 ImagesSynonyms: ZD1694 (Standard); D1694 (Standard); ICI-D1694 (Standard)Raltitrexed (Standard) is the analytical standard of Raltitrexed. This product is intended for research and analytical applications. Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase.
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CB 3703
0 ImagesCat. No.: HY-119143CAS No.: 32093-09-7CB 3703 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR). CB 3703 has an IC50 of 0.25 μM against rat TS, a Ki of 0.47 μM against mouse TS, an IC50 of 6.8 nM against rat DHFR, and a Ki of 0.6 pM against mouse DHFR. CB 3703 is transported via the reduced folate pathway, has a short plasma half-life, and can prolong the survival of tumor-bearing mice. CB 3703 can be used in the research of L1210 ascites tumors.
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N-Acetyl-4-S-cysteaminylphenol
0 ImagesCat. No.: HY-W129441CAS No.: 91281-32-2Synonyms: N-Ac-4-S-CAPN-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.
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BGC638
0 ImagesCat. No.: HY-165280CAS No.: 416852-27-2BGC638 is a thymidylate synthase inhibitor with a Ki value of 0.24 nM. BGC638 binds to α-FR with high affinity and enters cells via receptor-mediated endocytosis, thereby potently inhibiting thymidylate synthase to block DNA synthesis and ultimately induce apoptosis. BGC638 is applicable to studies related to α-FR-overexpressing tumors and epithelial carcinomas (ovarian cancer and endometrial cancer).
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Folitixorin sodium
0 ImagesCat. No.: HY-14769BCAS No.: 133978-76-4Synonyms: 5,10-Methylenetetrafolate sodium; ANX-510 sodiumFolitixorin sodium (5,10-Methylenetetrafolate sodium; ANX-510 sodium) is a reduced form of Folic acid (HY-16637) and a cofactor of thymidylate synthase. Folitixorin sodium 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 sodium in combination with 5-fluorouracil and αVEGF reduces tumor volume in colorectal tumor models of nude mice. Folitixorin sodium is used in related research on Yoshida sarcoma, P-388 leukemia, and colorectal cancer.
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Fosifloxuridine nafalbenamide (Standard)
0 ImagesCat. No.: HY-109115RCAS No.: 1332837-31-6Synonyms: NUC-3373 (Standard)Fosifloxuridine nafalbenamide (Standard) is the analytical standard of Fosifloxuridine nafalbenamide (HY-109115). This product is intended for research and analytical applications. 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 immunoresearch.
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5-Fluoroorotic acid (Standard)
0 Images5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity.
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Diazaquinomycin A
0 ImagesCat. No.: HY-N14161CAS No.: 87614-40-2Diazaquinomycin 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.
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SB-328437 (Standard)
0 ImagesCat. No.: HY-103363RCAS No.: 247580-43-4SB-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.
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TS-IN-7
0 ImagesCat. No.: HY-178288CAS No.: 150585-99-2TS-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.
