60477-34-1

60477-34-1 structure

Name: Pifithrin-β
Chemical Name: 2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
CAS Number: 60477-34-1
Molecular Formula: C₁₆H₁₆N₂S
Molecular Weight: 268.37700
Catalog: Signaling Pathways Apoptosis MDM-2/p53
Create Date: 2017-01-22 08:20:30
Modify Date: 2024-01-01 19:40:24
Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.

Name	2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
Synonyms	Pifithrin-Beta UNII-45I8QO7K37 Pifithrin-β

Description	Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.
Related Catalog	Signaling Pathways >> Apoptosis >> MDM-2/p53 Research Areas >> Cancer
Target	IC50: 23 μM (p53)[1]
In Vitro	Pifithrin-α, an inhibitor of the p53 protein, is regarded as a lead compound for cancer and neurodegenerative disease therapy. Pifithrin-α is very unstable in culture medium and rapidly converts to its condensation product pifithrin-β, the N-acetyl derivative[2]. After 24 h, the viability assay shows that the pretreatments with 1 and 10 μM pifithrin-β exerts neuroprotective effects[3].
References	[1]. Christodoulou MS, et al. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg Med Chem. 2011 Mar 1;19(5):1649-57. [2]. Fernández-Cruz ML, et al. Biological and chemical studies on aryl hydrocarbon receptor induction by the p53 inhibitor pifithrin-α and its condensation product pifithrin-β. Life Sci. 2011 Apr 25;88(17-18):774-83. [3]. Da Pozzo E, et al. p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. ACS Chem Neurosci. 2014 May 21;5(5):390-9.