Home Metabolism P450 (e.g. CYP17) inhibitor Thiabendazole

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Thiabendazole P450 (e.g. CYP17) inhibitor

Cat.No.S1739

Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).
Thiabendazole P450 (e.g. CYP17) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 201.25

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Quality Control

Batch: S173901 DMSO]40 mg/mL]false]Ethanol]1 mg/mL]false]Water]Insoluble]false Purity: 100%
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100

Solubility

In vitro
Batch:

DMSO : 40 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 201.25 Formula

C10H7N3S

 Storage (From the date of receipt)
CAS No. 148-79-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C2C(=C1)NC(=N2)C3=CSC=N3

Mechanism of Action

Targets/IC50/Ki
CYP1A2
In vitro
Thiabendazole provokes a strong DNA-damaging activity in the human lymphoblastoid cell line that constitutively expresses human CYP1A1 cDNA, but not in the parental line, indicating that CYP1A1 is chiefly implicated in carbaryl and thiabendazole genotoxicity. This compound provokes a dose- and time-dependent increase in CYP1A1 (EROD activity, protein and mRNA levels) in primary culture of rat hepatocytes. It results in the induction of 7-ethoxyresorufin O-deethylase and 7-pentoxyresorufin O-depentylase activities, CYP1A1, CYP1A2, CYP2B1 and CYP2B1/2 mRNA levels and CYP1A2 and CYP2B1/2 apoprotein levels. This chemical markedly induces GSTP1 mRNA levels, but has only a small effect on GSTT1 mRNA levels. It is rapidly transported by passive diffusion through the human intestinal cells by comparison with the protein-bound residues which are not able to cross the intestinal barrier. It will be firstly metabolized to 5OH-TBZ and subsequently converted to a chemically reactive metabolic intermediate binding to proteins.
In vivo
Thiabendazole results in nephrosis or hydronephrosis and this organ toxicity may lead to the high dose-dependent mortality in treated mice. This compound results in hormone imbalance and this imbalance may play an important role in the changes of the reproductive or endocrine system in treated mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10936227/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11718957/
  • [6] https://pubmed.ncbi.nlm.nih.gov/16261361/

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