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

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Alternate Names:
Pifithrin-α hydrobromide is also known as PFT-α.
Application:
Pifithrin-α hydrobromide is an inhibitor of p53 that reversibly blocks p53 dependent transcriptional activation and apoptosis.
CAS Number:
63208-82-2
Purity:
≥98%
Molecular Weight:
367.30
Molecular Formula:
C16H18N2OS•HBr
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Pifithrin-α hydrobromide 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. Additionally, Pifithrin-α is an aryl hydrocarbon receptor (AHR) agonist, which leads to the upregulation of AHR target gene CYP1A1 (EC50 = 1.1 µM). Uses of pifithrin-α hydrobromide extend to the study of cellular resilience and adaptability in response to environmental stresses. Researchers can study how modulation of transcription factor activities can impact cellular decision-making processes, including survival, adaptation, and response to external signals.


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

  1. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.  |  Komarov, PG., et al. 1999. Science. 285: 1733-7. PMID: 10481009
  2. Suppression of p53: a new approach to overcome side effects of antitumor therapy.  |  Komarova, EA. and Gudkov, AV. 2000. Biochemistry (Mosc). 65: 41-8. PMID: 10702639
  3. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid beta-peptide.  |  Culmsee, C., et al. 2001. J Neurochem. 77: 220-8. PMID: 11279278
  4. Doxorubicin induces apoptosis and CD95 gene expression in human primary endothelial cells through a p53-dependent mechanism.  |  Lorenzo, E., et al. 2002. J Biol Chem. 277: 10883-92. PMID: 11779855
  5. p53 is a determinant of X-linked inhibitor of apoptosis protein/Akt-mediated chemoresistance in human ovarian cancer cells.  |  Fraser, M., et al. 2003. Cancer Res. 63: 7081-8. PMID: 14612499
  6. The p53 inhibitor pifithrin-alpha is a potent agonist of the aryl hydrocarbon receptor.  |  Hoagland, MS., et al. 2005. J Pharmacol Exp Ther. 314: 603-10. PMID: 15843497
  7. Pifithrin-alpha protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53.  |  Sohn, D., et al. 2009. Cell Death Differ. 16: 869-78. PMID: 19229248
  8. Signalling pathways involved in antitumoral effects of VIP in human renal cell carcinoma A498 cells: VIP induction of p53 expression.  |  Vacas, E., et al. 2014. Int J Biochem Cell Biol. 53: 295-301. PMID: 24905957
  9. Semaphorin 3E regulates apoptosis in the intestinal epithelium during the development of colitis.  |  Eissa, N., et al. 2019. Biochem Pharmacol. 166: 264-273. PMID: 31170375
  10. The glycoprotein mucin-1 negatively regulates GalNAc transferase 5 expression in pancreatic cancer.  |  Caffrey, T., et al. 2019. FEBS Lett. 593: 2751-2761. PMID: 31283009
  11. P53/PANK1/miR-107 signalling pathway spans the gap between metabolic reprogramming and insulin resistance induced by high-fat diet.  |  Yang, L., et al. 2020. J Cell Mol Med. 24: 3611-3624. PMID: 32048816
  12. Triptolide enhances lipolysis of adipocytes by enhancing ATGL transcription via upregulation of p53.  |  Wang, X., et al. 2020. Phytother Res. 34: 3298-3310. PMID: 32614500
  13. The transcriptional cofactor Jab1/Cops5 is crucial for BMP-mediated mouse chondrocyte differentiation by repressing p53 activity.  |  Mamidi, MK., et al. 2021. J Cell Physiol. 236: 5686-5697. PMID: 33393086
  14. p53 Promotes Ferroptosis in Macrophages Treated with Fe3O4 Nanoparticles.  |  Wu, C., et al. 2022. ACS Appl Mater Interfaces. 14: 42791-42803. PMID: 36112832
  15. Angiotensin II-induced vascular endothelial cells ferroptosis via P53-ALOX12 signal axis.  |  Liu, C., et al. 2023. Clin Exp Hypertens. 45: 2180019. PMID: 36860117

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Pifithrin-α hydrobromide, 5 mg

sc-45050
5 mg
$118.00

Pifithrin-α hydrobromide, 25 mg

sc-45050A
25 mg
$287.00

How do you reconstitute the powder?

Asked by: animeshu11
Thank you for your question. It would be helpful if you could call us directly at 800-457-3801ext.1, allowing for a more interactive discussion of this and other related questions.
Answered by: Blake J
Date published: 2021-11-23

Is this product cell permeable?

Asked by: SCchem16
Thank you for your question. This chemical, Pifithrin-α hydrobromide: sc-45050, is a cell-permeable chemical inhibitor of p53.
Answered by: Chemical Support 2
Date published: 2017-04-05

What are the recommended conditions for long term storage?

Asked by: SCchem16
Thank you for your question. For this chemical, Pifithrin-α hydrobromide (CAS 63208-82-2), we recommend this be stored long-term at -20ºC and away from light and moisture.
Answered by: Chemical Support 2
Date published: 2017-04-05
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Rated 5 out of 5 by from LuoLuo, et. al. (PubMed ID 19475672) used Pifithrin- hydrobromide, a p53 inhibitor, to treat rats post middle cerebral artery occlusion. They found that p53 was indeed reduced. -SCBT Publication Review
Date published: 2015-01-25
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Pifithrin-α hydrobromide is rated 5.0 out of 5 by 1.
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