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Apoptosis——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.

Apoptosis——Thymidylate Synthase(8)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM7972 Fosifloxuridine nafalbenamide

Fosifloxuridine nafalbenamide (NUC-3373) 属于嘧啶核苷酸类似物,是一种胸腺嘧啶合酶 (Thymidylate synthase) 抑制剂。Fosifloxuridine nafalbenamide 具有抗癌活性。Fosifloxuridine nafalbenamide 具有诱发宿主免疫反应和增强免疫治疗的潜力。

1332837-31-6 98%
KM3946 Nolatrexed dihydrochloride

Nolatrexed dihydrochloride (AG 337) 是一种非竞争性的胸苷酸合酶 (thymidylate synthase) 抑制剂,与该酶的叶酸辅因子结合位点相互作用,对人 thymidylate synthase 的 Ki 值为 11 nM。Nolatrexed dihydrochloride (AG 337) 能够在癌细胞 S 期诱导细胞周期停滞。具有抗癌活性。

152946-68-4 98%
KM7397 Nolatrexed-d4 dihydrochloride

Nolatrexed-d4 dihydrochloride 是 Nolatrexed dihydrochloride 的氘代物。Nolatrexed dihydrochloride (AG 337) 是一种非竞争性的胸苷酸合酶 (thymidylate synthase) 抑制剂,与该酶的叶酸辅因子结合位点相互作用,对人 thymidylate synthase 的 Ki 值为 11 nM。Nolatrexed dihydrochloride (AG 337) 能够在癌细胞 S 期诱导细胞周期停滞。具有抗癌活性。

KM3396 ONX 0801 trisodium

ONX 0801 (BGC 945) trisodium 是胸腺激酶合成酶 (TS) 的抑制剂,靶向α 叶酸受体过表达的肿瘤。

1097638-00-0
KM9754 Raltitrexed

Raltitrexed是一种用于化疗的抗代谢药物,通过抑制胸苷酸合成酶起作用。

112887-68-0 98%
KM19470 Tipiracil

Tipiracil 是一种胸苷磷酸化酶 (TPase) 抑制剂。

183204-74-2
KM17960 Trifluridine

Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) 是不可逆的胸苷酸合酶抑制剂,从而抑制 DNA合成。Trifluridine 是用于单纯疱疹病毒 (HSV) 感染的抗病毒药物。

70-00-8 99%
KM11597 Trifluridine/tipiracil hydrochloride mixture

Trifluridine-tipiracil hydrochloride mixture (TAS-102) 是一种新型的口服组合药物。由基于胸苷的抗肿瘤核苷类似物,三氟胸苷和有效的胸苷磷酸化酶 (thymidine phosphorylase) 抑制剂派替西西以1比0.5比例组成。

733030-01-8 ≥98%
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