Pifithrin-alpha hydrobromide An inhibitor of p53 that reversibly blocks p53 dependent transcriptional activation and apoptosis

Pifithrin-α hydrobromide (CAS 63208-82-2)

  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getAggregateRating, 69ms
  • REVIEWS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
Sinónimo: PFT-α; 1-(4-Methylphenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)ethanone hydrobromide
Solicitud: An inhibitor of p53 that reversibly blocks p53 dependent transcriptional activation and apoptosis
Número de CAS: 63208-82-2
Pureza: ≥98%
Peso Molecular: 367.30
Fórmula Molecular: C16H18N2OS•HBr
* En el Certificado de Análisis específico de lote, puede encontrar información específica (como el contenido en agua).
Envíe una reseña para este producto y reciba 15 créditos Cruz

Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. It enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin (sc-280681), etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation, and does not induce visible tumors. Protects against neuronal death in models of stroke and neurodegenerative disorders. Pifithrin-α is also an aryl hydrocarbon receptor (AHR) agonist, which leads to the upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).


References

1. Komarov, P G., et al., 1999. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science (New York, N.Y.). 285(5434): 1733-7. PMID: 10481009
2. Komarova, E A., et al., 2000. Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry. Biokhimia. 65(1): 41-8. PMID: 10702639
3. Culmsee, C., et al., 2001. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid beta-peptide. Journal of neurochemistry. 77(1): 220-8. PMID: 11279278
4. Lorenzo, Elisa., et al., 2002. Doxorubicin induces apoptosis and CD95 gene expression in human primary endothelial cells through a p53-dependent mechanism. The Journal of biological chemistry. 277(13): 10883-92. PMID: 11779855
5. Hoagland, Martin S., et al., 2005. The p53 inhibitor pifithrin-alpha is a potent agonist of the aryl hydrocarbon receptor. The Journal of pharmacology and experimental therapeutics. 314(2): 603-10. PMID: 15843497
6. Sohn, D., et al., 2009. Pifithrin-alpha protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53. Cell death and differentiation. 16(6): 869-78. PMID: 19229248

Estado de Materia :
Solid
Solubilidad :
Soluble in DMSO (20 mg/ml), water, DMF (~1 mg/ml), 1:10 DMSO:PBS (pH 7.2) (~ 0.1 mg/ml), 100% ethanol, and methanol. Sparingly soluble in aqueous buffers.
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
192.1-192.5° C
IC50 :
CYP1A1 upregulation: EC5050 = 1.1 µM
Valores de pK :
pKb: 3.19 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
9929138
Indice de Merck :
14: 7421
Número MDL :
MFCD00417851
SMILES :
CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br

Descargar SDS (MSDS)

CERTIFICADO DE ANÁLISIS

Necesita Adobe Acrobat Reader para ver de forma fiable,
imprimir y comentar el documento de PDF

Pifithrin-alpha hydrobromide  Menciones del Producto

Ver como otros han utilizado Pifithrin-alpha hydrobromide. Haga click en la entrada de PubMed .

Citaciones 1 a 10 de un total de 23

PMID: # 28608259  Qiu, M. et al. 2017. Cancer Chemother. Pharmacol. 80: 275-286.

PMID: # 27464000  Zhang, Y. et al. 2016. Autophagy. 12: 1538-59.

PMID: # 26884717  Yu, W. et al. 2016. Int. J. Biol. Sci. 12: 198-209.

PMID: # 26431790  Yin, R. et al. 2016. Respir Physiol Neurobiol. 220: 81-7.

PMID: # 25466893  Liu, W. et al. 2015. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 29: 1113-23.

PMID: # 25727698  Wang, Y. et al. 2015. J. Neurochem. 133: 828-43.

PMID: # 24722580  Moretti, RM. et al. 2014. PloS one. 9: e93713.

PMID: # 25193078  Das, A. et al. 2014. Exp. Cell Res. 328: 361-78.

PMID: # 24946002  Sun, H. et al. 2014. Br. J. Cancer. 111: 281-91.

PMID: # 21521785  Verma, S. et al. 2011. Blood. 117: 6600-7.

Citaciones 1 a 10 de un total de 23
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getContent, 99ms
  • QUESTIONS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getReviews, 40ms
  • REVIEWS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;

Santa Cruz Biotechnology, Inc. es un líder mundial en el desarrollo de productos para el mercado de la investigación biomédica. Llámenos gratis al 00 800 4573 8000.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved."Santa Cruz Biotechnology", y el logo de Santa Cruz Biotechnology, Inc., "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", el logo de San Juan Ranch, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", y "EZ Touch" son marcas registradas de Santa Cruz Biotechnology, Inc. Todas las marcas registradas son propiedad de su respectivo dueño.