A ribonucleotide reductase inhibitor and iron chelator with antitumor activity; inhibits DNA synthesis and repair by destroying the tyrosine free radical in the R2/p53R2 subunits of ribonucleotide reductase through the formation of a redox active complex with iron

3-AP – 5 mg

Brand:
Cayman
CAS:
143621-35-6
Storage:
-20
UN-No:
Non-Hazardous - /

Ribonucleotide reductase, the rate-limiting enzyme for de novo DNA synthesis, is an excellent target for chemotherapy. Its increased activity in cancer cells is associated with malignant transformation and proliferation.{14245} 3-AP is a ribonucleotide reductase inhibitor and iron chelator with antitumor activity.{25052} At 5 μM it can enhance DU145, U251, and PSN1 tumor cell radiosensitivity in vitro, inhibiting DNA synthesis and repair.{25052} It destroys the tyrosine free radical in the R2/p53R2 subunits of ribonucleotide reductase by forming a redox active complex with iron, thus producing reactive oxygen species.{25051} Furthermore, 3-AP has been shown to activate an endoplasmic reticulum stress pathway, leading to the unfolded protein response and apoptosis.{25050}  

 

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Description

A ribonucleotide reductase inhibitor and iron chelator with antitumor activity; inhibits DNA synthesis and repair by destroying the tyrosine free radical in the R2/p53R2 subunits of ribonucleotide reductase through the formation of a redox active complex with iron

Formal name: 2-[(3-amino-2-pyridinyl)methylene]-hydrazinecarbothioamide

Synonyms:  3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone|NSC 663249|Triapine™

Molecular weight: 195.2

CAS: 143621-35-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Metal Chelators||Product Type|Biochemicals|Nucleotides/Nucleosides||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|DNA Damage and Repair||Research Area|Cancer|Metabolism||Research Area|Oxidative Stress & Reactive Species|Pro-oxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen

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