Thymidylate synthase (TSase) is an important enzyme for cell growth because it catalyzes a process required for DNA replication by reductively methylating the co-substrate N5,N10-methylene-5,6,7,8-tetrahydrofolate (CH2H4F) to produce 2′-deoxythymidine-5′-monophosphate (dTMP).
Throughout the cell cycle, TSase activity and expression are tightly regulated, particularly at the translational level. By physically attaching to the TSase mRNA at both the translational start site (TSS) and the coding region, the TSase protein prevents the message from being translated. Additionally, TSase can bind to the mRNA of at least nine additional significant gene products, including those of p53 and c-myc. As a result, altering the level of the TSase protein may have a series of repercussions on cell growth. The synthesis and repair of DNA precursors depend on TSase, which has established itself as a key target for numerous chemotherapeutic and antibiotic drugs. The use of structural analogs of dUMP and CH2H4F as thymidylate synthase inhibitors is well-established. Examples include fluoropyrimidines and antifolates.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V51752 | DG1 (Compound 8Nc) | Thymidylate Synthase (TS) inhibitor | |
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V17929 | Leucovorin (Folinic acid) | 58-05-9 | Leucovorin (Folinic acid), the active metabolite of folic acid, is used primarily as the calcium salt form as an antidote/rescue agent to folic acid antagonists which block the conversion of folic acid to folinic acid. |
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V76060 | MtTMPK-IN-2 | 2799607-71-7 | MtTMPK-IN-2 (compound 15) is a potent inhibitor of mycobacterial thymidylate kinase (MtbTMPK) with IC50 of 1.1 μM. |
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V76059 | MtTMPK-IN-3 | 2799607-80-8 | MtTMPK-IN-3 (compound 25) is a potent inhibitor of mycobacterial thymidylate kinase (MtbTMPK) with IC50 of 0.12 μM. |
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V16389 | Nolatrexed 2HCl | 152946-68-4 | Nolatrexed dHCl (AG-337 dihydrochloride;thymitaq),afolateanalog,is a novel and potent thymidylate synthase inhibitorwith potential anticancer activity. |
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V32163 | Tipiracil | 183204-74-2 | Tipiracil (TPI), one of the key components inTAS-102 (trade name Lonsurf, a mixture of Trifluridine and tipiracil hydrochloridein a 1:0.5 molar ratio), is a potent thymidine phosphorylase (TPase) inhibitor with anticancer activity. |
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V13525 | Tipiracil HCl | 183204-72-0 | Tipiracil HCl (formerly known as TPI; TAS-1-462, MA-1; trade name Lonsurf), the hydrochloride salt of tipiracil,is a thymidine phosphorylase inhibitor (TPI) approved for use in combination(TAS-102) with trifluridinefor cancer treatment. |
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