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Pifithrin-α hydrobromide
- PFT-α
- Parent CAS: 206983-57-5
- Soluble in DMSO
- MF: C16H18N2OS.HBr
- MW: 367.3
Description
Pifithrin-α hydrobromide is a reversible p53 pathway inhibitor that blocks p53-dependent transcriptional activation and apoptosis in DNA damage response models.
p53 controls transcriptional programs involved in cell-cycle arrest, apoptosis, senescence and genomic stress responses. Pifithrin-α is used to distinguish p53-dependent cellular outcomes from p53-independent apoptosis and stress pathways.
Key Features
- Reversible p53 pathway inhibitor
- Blocks p53-dependent transcriptional activation
- Suppresses DNA damage-induced p53-dependent apoptosis
- Useful for separating p53-dependent and p53-independent stress responses
Applications
- p53 transcriptional activity assays
- DNA damage response research
- Apoptosis and cell-survival studies
- TP53 pathway validation experiments
Note: Pifithrin-α is unstable in vitro and is rapidly converted to Pifithrin-β (Axon 3051).
More Information
| Parent CAS No. | 206983-57-5 |
|---|---|
| Chemical Name | 2-(2-imino-4,5,6,7-tetrahydrobenzo[d]thiazol-3(2H)-yl)-1-p-tolylethanone hydrobromide |
| SMILES | C1CC2SC(=N)N(CC(=O)C3C=CC(C)=CC=3)C=2CC1.Br |
| MFCD | MFCD00417851 |
| InChi | InChI=1S/C16H18N2OS.BrH/c1-11-6-8-12(9-7-11)14(19)10-18-13-4-2-3-5-15(13)20-16(18)17;/h6-9,17H,2-5,10H2,1H3;1H |
| InChiKey | HAGVCKULCLQGRF-UHFFFAOYSA-N |
| CID | 9929138 |
| Short Description | p53 inhibitor |
References
- PG Komarov et al. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science. 1999, 285(5434), 1733-7.
- PJM Murphy et al. Pifithrin-α Inhibits p53 Signaling after Interaction of the Tumor Suppressor Protein with hsp90 and Its Nuclear Translocation. J. Biol. Chem. 2004, 279, 30195-30201.
- D Sohn et al. Pifithrin-α protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53. Cell Death and Differentiation. 2009, 16, 869–878.
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