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| | CYCLIC-PIFITHRIN-ALPHA Basic information |
| Product Name: | CYCLIC-PIFITHRIN-ALPHA | | Synonyms: | Pifithrin-α, Cyclic- - CAS 60477-34-1 - Calbiochem;Pifithrin-alpha (cyclic) . HBr;5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazole;Pifithrin-2;Imidazo[2,1-b]benzothiazole, 5,6,7,8-tetrahydro-2-(4-methylphenyl)-;Pifithrin-β (QB-102 and Cyclic-Pifithrin-α);2-(p-Tolyl)-5,6,7,8-tetrahydrobenzo[d]imidazo[2,1-b]thiazole;Pifithrin-α, Cyclic- - CAS 60477-34-1 - Calbiochem | | CAS: | 60477-34-1 | | MF: | C16H16N2S | | MW: | 268.38 | | EINECS: | | | Product Categories: | | | Mol File: | 60477-34-1.mol |  |
| | 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 |
| WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | 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. |
| | CYCLIC-PIFITHRIN-ALPHA Preparation Products And Raw materials |
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