| Identification | Back Directory | [Name]
CYCLIC-PIFITHRIN-ALPHA | [CAS]
60477-34-1 | [Synonyms]
Pifithrin-2
Pifithrin-alpha (cyclic) . HBr
Pifithrin-β (QB-102 and Cyclic-Pifithrin-α)
Pifithrin-α, Cyclic- - CAS 60477-34-1 - Calbiochem
5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazole
Imidazo[2,1-b]benzothiazole, 5,6,7,8-tetrahydro-2-(4-methylphenyl)- | [Molecular Formula]
C16H16N2S | [MDL Number]
MFCD02108837 | [MOL File]
60477-34-1.mol | [Molecular Weight]
268.38 |
| Chemical Properties | Back Directory | [Melting point ]
266.4-267.3 °C(lit.) | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C | [solubility ]
DMSO: 20 mg/mL | [form ]
White solid | [pka]
6.75±0.20(Predicted) | [color ]
white |
| Hazard Information | Back Directory | [Uses]
Pifithrin-β (PFT β) is a potent p53 inhibitor with an IC50 of 23 μM. | [Definition]
ChEBI: 2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole is a member of imidazoles. | [General Description]
A cell-permeable and very stable analog of Pifithrin-α (Cat. No. 506132), with similar biological function, but with reduced cytotoxicity. A chemical inhibitor of p53. Reversibly inhibits p53-dependent transactivation of p53-responsive genes; also reversibly blocks p53-mediated apoptosis. Acts as a P-gp modulator by changing relative substrate specificity of the transporter. This compound has been reported to be a potent STAT6 transcriptional inhibitor. | [Biochem/physiol Actions]
Cell permeable: yes | [storage]
Store at -20°C | [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. DOI:10.1016/j.bmc.2011.01.039
[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. DOI:10.1016/j.lfs.2011.02.019
[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. |
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