Pifithrin-ɑ

• CAT Number: I004381
• CAS Number: 63208-82-2
• Molecular Formula: C16H18N2OS HBr
• Molecular Weight: 367.3
• Purity: ≥95%
• Synonyms: 2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-methylphenyl)ethanone;hydrobromide
• Target: p53
• Solubility: DMSO: ≥ 43 mg/mL
• Storage: Store at -20°C
• 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
• SMILES: CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br

Pifithrin-α (CAT: I004381) is a small molecule compound that has been extensively studied for its potential as a p53 inhibitor. Pifithrin-α specifically targets and inhibits the transcriptional activity of the tumor suppressor protein p53. By inhibiting p53, Pifithrin-α can interfere with the downstream signaling pathways involved in cell cycle arrest, DNA repair, and apoptosis. It has been used in various research settings to investigate the role of p53 in cellular processes and disease models. Pifithrin-α has shown potential therapeutic applications in cancer treatment by sensitizing p53-mutated cancer cells to chemotherapy and radiation therapy. It may also have neuroprotective effects in certain neurodegenerative disorders.

Reference

1: Kanno S, Kurauchi K, Tomizawa A, Yomogida S, Ishikawa M. Pifithrin-alpha has a
p53-independent cytoprotective effect on docosahexaenoic acid-induced
cytotoxicity in human hepatocellular carcinoma HepG2 cells. Toxicol Lett. 2015
Jan 22;232(2):393-402. doi: 10.1016/j.toxlet.2014.11.016. Epub 2014 Nov 18.
PubMed PMID: 25448278.

2: Fetoni AR, Bielefeld EC, Paludetti G, Nicotera T, Henderson D. A putative role
of p53 pathway against impulse noise induced damage as demonstrated by protection
with pifithrin-alpha and a Src inhibitor. Neurosci Res. 2014 Apr-May;81-82:30-7.
doi: 10.1016/j.neures.2014.01.006. Epub 2014 Jan 25. PubMed PMID: 24472721.

3: Dorofeeva NA, Chernigovskaya EV, Nikitina LS, Glazova M. Effect of p53
inhibition by pifithrin-alpha on functional activity of vasopressin neurones in
rat hypothalamus. Ross Fiziol Zh Im I M Sechenova. 2013 Aug;99(8):901-16. PubMed
PMID: 25470941.

4: Ng LT, Wu SJ. Antiproliferative Activity of Cinnamomum cassia Constituents and
Effects of Pifithrin-Alpha on Their Apoptotic Signaling Pathways in Hep G2 Cells.
Evid Based Complement Alternat Med. 2011;2011:492148. doi: 10.1093/ecam/nep220.
Epub 2011 May 2. PubMed PMID: 20038571; PubMed Central PMCID: PMC3135661.