货号 | 15419-1mg |
描述 | 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.1 3-AP is a ribonucleotide reductase inhibitor and iron chelator with antitumor activity.2 At 5 μM it can enhance DU145, U251, and PSN1 tumor cell radiosensitivity in vitro, inhibiting DNA synthesis and repair.2 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.3 Furthermore, 3-AP has been shown to activate an endoplasmic reticulum stress pathway, leading to the unfolded protein response and apoptosis.4 |
别名 | 3-Aminopyridine-2-Carboxyaldehyde Thiosemicarbazone;NSC 663249;Triapine™; |
供应商 | Cayman |
应用文献 | |
1.Szekeres, T.,Fritizer, M.,Strobl, H., et al. Synergistic growth inhibitory and differentiating effects of trimidox and tiazofurin in human promyelocytic leukemia HL-60 cells. Blood 84(12), 4316-4321 (1994). 2.Barker, C.A.,Burgan, W.E.,Carter, D.J., et al. In vitro and in vivo radiosensitization induced by the ribonucleotide reductase inhibitor triapine (3-aminopyridine-2-carboxaldehyde-thiosemicarbazone). Clinical Cancer Research 12(9), 2912-2918 (2006). 3.Chapman, T.R. and Kinsella, T.J. Ribonucleotide reductase inhibitors: A new look at an old target for radiosensitization. Front.Oncol. 1, 56 (2012). 4.Trondl, R.,Flocke, L.S.,Kowol, C.R., et al. Triapine and a more potent dimethyl derivative induce ER stress in cancer cells. Molecular Pharmacology 85(3), 451-459 (2013). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 195.2 |
分子式 | C7H9N5S |
CAS号 | 143621-35-6 |
稳定性 | ≥ 2 years |
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