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HOME> Products> Natural and Chemical compound> Enzyme inhibitor> Vanoxonin [CAS: 86933-99-5]

Thymidylate Synthase Inhibitor Vanoxonin [CAS: 86933-99-5]

Date：July 03 2020Web Page No：520048

Vanoxonin is found in cultured broth of Saccharopolyspora hirsuta MG245-CF2 as an inhibitor of thymidylate synthetase^1,2). Vanoxonin forms a vanadium (V⁵⁺) complex which exhibits a strong inhibition against the synthetase¹⁾. The structure-activity rerationship has been studied³⁾.

What is Thymidylate Synthase
Specification
Application Note
Reference

What is Thymidylate Synthase

Thymidylate synthase (TS) is a key enzyme, which is responsible for the reductive methylation of deoxyuridylic acid (dUMP) to deoxythymidylic acid (dTMP). The methylation of the uracil moiety to 5-methyl uracil (thymine) requires participation of a folic acid coenzyme, N⁵, N¹⁰-methylenetetrahydrofolate as a methyl donor. The functioning of thymidylate synthetase is coupled with the activity of dihydrofolate reductase (DHF reductase). That is why this biochemical target is usually referred to as thymidylate synthetase/ DHF reductase⁴⁾.

DNA-producing cells require large amounts of thymidylate synthase to facilitate DNA production. In S and G₂ phases of cell cycle, more thymidylate synthase (>20%) is produced. Thymidylate synthase has been studied as a candidate tumor marker in some cancers, such as gastrointestinal tract (stomach, rectum etc.) ⁵⁾.

Thymidylate Synthase Inhibitors — Thymidylate synthase inhibitors

Reference

Sharma, S. and Anand, N., "Approaches to Design and Synthesis of Antiparasitic Drugs", in Pharmacochemistry Library, 6th Edition (1997), Elsevier.
Chernecky, C.C. and Berger, B.J., in Laboratory Tests and Diagnostic Procedures (2013), Elsevier.

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Specification

CAS#	86933-99-5
Molecular Formula	C₁₈H₂₅N₃O₉
Molecular Weight	427.41
Source	Saccharopolyspora hirusta MG245-CF2
Purity	>80% (HPLC)
Solubility	Soluble in MeOH, DMSO, Acetic Acid and H₂O Insoluble in Ethyl acetate, CHCl₃ and n-Hexane

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Application Note

Vanoxonin-V⁵⁺ complex inhibits thymidylate synthetase (IC₅₀: 0.7 µg/mL), however vanoxonin alone shows IC₅₀: 200 µg/mL only¹⁾.
Vanoxonin-V⁵⁺ complex shows in vitro cytotoxic activity against L-1210 lymphatic leukemia cells (MIC: 25 µg/mL) ¹⁾.

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Reference

Kanai F., et al., J. Antibiot., 36 (6), 656～660 (1983). [PMID:6874588]
Kanai F., et al., J. Antibiot., 38 (1), 31～38 (1985). [PMID:3972726]
Kanai F., et al., J. Antibiot., 38 (1), 39～50 (1985). [PMID:3972727]

[Date : April 25 2025 00:06]

Detail Product Name Product Code Supplier Size Price

Vanoxonin, Thymidylate Synthase Inhibitor
DatasheetThis may not be the latest data sheet. 10744 IMCInstitute of Microbial Chemistry 1 mg $500

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Description
Storage	-20°C	CAS	86933-99-5
Link	Bioactive Compounds

[Date : April 25 2025 00:06]

Vanoxonin, Thymidylate Synthase Inhibitor

DatasheetThis may not be the latest data sheet.

Product Code: 10744
Supplier: IMC
Size: 1mg
Price: $500

Description
Storage	-20°C	CAS	86933-99-5
Link	Bioactive Compounds

Contact

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