CYCLIC-PIFITHRIN-ALPHA Chemical Properties

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

Safety Information

WGK Germany 

3

CYCLIC-PIFITHRIN-ALPHA Usage And Synthesis

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

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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