Cyclic Pifithrin-α hydrobromide

Cat. No. 3843

Cyclic Pifithrin-a hydrobromide C16H16N2S.HBr [511296-88-1]

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Alternative Name: Pifithrin-β

Chemical Name: 5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazole hydrobromide

Biological Activity

Cyclic analog of pifithrin-α (Cat. No. 1267), a small molecule inhibitor of p53. Prevents dexamethasone-induced cell death in murine thymocytes (EC50 = 2.01 μM). Sensitizes p53-deficient tumors to radiotherapy and chemotherapy; increases apoptosis in target cells when used in combination with antimicrotubule agents.

Technical Data

M.Wt:
349.29
Formula:
C16H16N2S.HBr
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
511296-88-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Zuco and Zunino (2008) Cyclic Pifithrin-α sensitizes wild type p53 tumor cells to antimicrotubule agent-induced apoptosis. Neoplasia 10 587. PMID: 18516295.

Barchechath et al (2005) Inhibitors of apoptosis in lymphocytes: synthesis and biological evaluation of compounds related to pifithrin-α. J.Med.Chem. 48 6409. PMID: 16190767.

Pietrancosta et al (2005) Novel cyclized Pifithrin-alpha p53 inactivators: synthesis and biological studies. Bioorg.Med.Chem.Lett. 15 1561. PMID: 15745797.

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