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Submit ReviewPifithrin-α hydrobromide is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of cancer therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM). Cyclic analog available (Cat. No. 3843).
分子量 | 367.3 |
公式 | C16H18N2OS.HBr |
储存 | Desiccate at -20°C |
CAS Number | 63208-82-2 |
PubChem ID | 9929138 |
InChI Key | HAGVCKULCLQGRF-UHFFFAOYSA-N |
Smiles | Br.CC1=CC=C(C=C1)C(=O)CN1C(=N)SC2=C1CCCC2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.73 | 100 |
以下数据基于产品分子量 367.3。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.72 mL | 13.61 mL | 27.23 mL |
5 mM | 0.54 mL | 2.72 mL | 5.45 mL |
10 mM | 0.27 mL | 1.36 mL | 2.72 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
参考文献是支持产品生物活性的出版物。
Culmsee et al (2001) A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide. J.Neurochem. 77 220 PMID: 11279278
Hoagland et al (2005) The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor. J.Pharmacol.Exp.Ther. 314 603 PMID: 15843497
Komarov et al (1999) A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 285 1733 PMID: 10481009
Komarova and Gudkov (2000) Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry 65 41 PMID: 10702639
Abdelalim and Tooyama (2012) The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells. Biochem.Biophys.Res.Comm. 420 605 PMID: 22445757
If you know of a relevant reference for Pifithrin-α hydrobromide, please let us know.
关键词: Pifithrin-a hydrobromide, Pifithrin-a hydrobromide supplier, p53, inhibitors, inhibits, aryl, hydrocarbon, receptors, agonists, AHR, Transcription, Factors, Pifithrin-alpha, hydrobromide, Aryl, Hydrocarbon, Receptors, Stem, Cell, Signaling, Autophagy, 1267, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Pifithrin-α hydrobromide 的部分引用包括:
Guha et al (2015) Novel Pactamycin Analogs Induce p53 Dependent Cell-Cycle Arrest at S-Phase in Human Head and Neck Squamous Cell Carcinoma (HNSCC) Cells. PLoS One 10 e0125322 PMID: 25938491
Norlin et al (2018) The ATPase activity of Asna1/TRC40 is required for pancreatic progenitor cell survival. Development 145 PMID: 29180572
Li et al (2018) Zinc deficiency causes neural tube defects through attenuation of p53 ubiquitylation. Development 145 PMID: 30545932
Fraser et al (2006) Regulation of p53 and suppression of apoptosis by the soluble guanylyl cyclase/cGMP pathway in human ovarian cancer cells. Cell Commun Signal 25 2203 PMID: 16288207
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The inhibitor worked nicely, and the results were consistent. We are happy with the quality of the product.
Pifithrin-alpha were dissolved in DMSO and used at a final concentration of 40 µM for pifithrin-alpha according to previous studies in which 3-100 µM pifithrin-alpha.
We used the p53 inhibitor in order to tackle the p53 protein in-vitro for some cellular proliferation assays,
We are happy with the quality of the product and the assistance from the Tocris technical department. All our questions about the use of the product where answered within a few hours.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.