Synthases/Synthetases

Cat. No.

A49967

CAS No.

111113-73-6

8-Deazahomofolic acid

8-Deazahomofolic acid is a potent inhibitor of thymidylate synthase (TS) and other folate-related enzymes. This compound exhibits significant inhibitory activity against folate-dependent bacterial strains, including S. faecium and L. casei, as well as strains resistant to methotrexate. Additionally, 8-Deazahomofolic acid demonstrates cytotoxic effects on L1210 leukemia cells, with an IC50 value of 87.5 μM. It is valuable in the study of bacterial infections and cancer research, providing insights into therapeutic strategies targeting folate metabolism.

Cat. No.

A53989

CAS No.

112887-62-4

ICI 198583

ICI 198583 is a potent inhibitor of thymidylate synthase (TS), exhibiting a Ki value of 10 nM against both mouse and human TS. It acts as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM, demonstrating dose-dependent and persistent inhibition of TS activity in vivo. This compound is valuable for research applications in leukemia and other related studies targeting nucleotide synthesis pathways.

Cat. No.

A53992

CAS No.

1332837-31-6

Fosifloxuridine nafalbenamide

Synonyms: NUC-3373

Fosifloxuridine nafalbenamide is a thymidylate synthase inhibitor, functioning as a pyrimidine nucleotide analogue. This compound exhibits significant anticancer activity by disrupting nucleotide synthesis essential for DNA replication. Additionally, Fosifloxuridine nafalbenamide has potential applications in eliciting host immune responses, making it a valuable tool for research in immunology and cancer therapies.

Cat. No.

A53993

CAS No.

153537-73-6

Plevitrexed

Synonyms: ZD 9331; BGC9331

Plevitrexed is a potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM, primarily utilized in the treatment of gastric cancer. It is absorbed through the α-folate receptor and the reduced folate carrier, demonstrating its effectiveness in targeting cancer cells. Additionally, Plevitrexed features an alkyne group, making it suitable for click chemistry applications, specifically in copper-catalyzed azide-alkyne cycloaddition (CuAAc), allowing for the functionalization of azide-containing molecules in biological research.

Cat. No.

A53995

CAS No.

61038-31-1

10-Formyl-5,8-dideazafolic acid

10-Formyl-5,8-dideazafolic acid is a potent inhibitor of thymidylate synthase. This compound is relevant in the study of nucleotide biosynthesis and cell proliferation, making it valuable in cancer research and the development of chemotherapeutic agents. Its inhibitory effect on thymidylate synthase underscores its potential in manipulating metabolic pathways associated with rapid cell division.

Cat. No.

A53999

CAS No.

501332-69-0

Idetrexed

Synonyms: BGC 945; ONX-0801; CB 300945

Idetrexed is a potent inhibitor of thymidylate synthase (TS) with a Ki of 1.2 nM. This compound demonstrates selective transport into α-folate receptor (α-FR)-overexpressing tumors, making it particularly relevant for research in ovarian cancer. Idetrexed is utilized in studies aimed at elucidating the mechanisms of TS inhibition and its therapeutic potential in cancer treatment.

Cat. No.

A54003

CAS No.

76849-19-9

CB 3717

Synonyms: PDDF

CB 3717 is a selective inhibitor of thymidylate synthase, competing with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). This compound also inhibits human dihydrofolate reductase, interacting competitively with dihydrofolate (Ki = 2.3 X 10(-8) M). In studies using WI-L2 human lymphoblastoid cells, CB 3717 significantly decreased dTTP levels while increasing dUMP levels, disrupting nucleotide metabolism. Its cytotoxic effects can be counteracted by thymidine supplementation, establishing thymidylate synthase as a rate-limiting factor in cellular proliferation. The timing of thymidine rescue is crucial, as delays beyond 8 hours lead to heightened toxicity in treated cells.

Cat. No.

A54005

CAS No.

102783-47-1

N,O-Didansyl-L-tyrosine cyclohexylammonium

N,O-Didansyl-L-tyrosine cyclohexylammonium is a selective inhibitor of thymidylate synthase (TS), effectively targeting TS in Escherichia coli, Lactobacillus casei, and human cells. It demonstrates potent inhibitory activity with IC50 values of 5.0 μM for E. coli, 3.4 μM for L. casei, and 119 μM for human TS. This compound serves as a valuable tool for studying thymidylate synthase in various biochemical and pharmaceutical research applications.

Cat. No.

A54006

CAS No.

1097638-00-0

Idetrexed trisodium

Synonyms: BGC 945 trisodium; ONX 0801 trisodium; CB 300945 trisodium

Idetrexed trisodium is a potent inhibitor of thymidylate synthase (TS) with a Ki of 1.2 nM. This compound is selectively transported into tumors that overexpress the alpha-folate receptor (α-FR), making it particularly relevant for research in ovarian cancer and other folate receptor-positive malignancies. It serves as a valuable tool for studying TS inhibition and exploring therapeutic strategies in cancer treatment.

Cat. No.

A54007

CAS No.

86933-99-5

Vanoxonin

Vanoxonin is a potent inhibitor of thymidylate synthase derived from Saccharopolyspora hirsuta, exhibiting an IC50 value of 0.7 μg/mL. This compound plays a crucial role in research applications focused on cancer therapeutics, particularly in the development of antimetabolites that target DNA synthesis. By disrupting thymidylate production, Vanoxonin may hinder cell proliferation in rapidly dividing cancer cells.

Cat. No.

A54009

CAS No.

157182-23-5

Metesind glucuronate

Synonyms: AG 331

Metesind glucuronate is a potent inhibitor of thymidylate synthase, exhibiting a Ki of 1.2 nM. By effectively disrupting DNA synthesis, it demonstrates significant anticancer activity, with an IC50 ranging from 0.4 to 0.9 μM. This compound is valuable for research applications focused on cancer therapeutics and cellular proliferation studies.

Cat. No.

A54010

CAS No.

145788-82-5

CB30900

CB30900 is a selective inhibitor of thymidylate synthase, demonstrating an IC50 of 0.2 μM. This compound exhibits significant cytotoxicity in the W1L2 cell line, with an IC50 value of 0.13 μM. It is valuable for research applications focusing on cancer biology and the mechanisms of nucleotide metabolism.