Pifithrin-β (QB-102 and Cyclic-Pifithrin-α)

Description: Pifithrin-beta (also known as QB102 and Cyclic-Pifithrin-alpha) is a novel and potent p53 inhibitor with an IC50 of 23 uM. It is a cell-permeable analog of Pifithrin-alpha but with higher stability and reduced cytotoxicity. Pifithrin-beta has neuroprotective activity by counteracting the Alzheimer peptide non-beta-amyloid component effects in human SH-SY5Y cells. The p53 is encoded in humans by the TP53 gene. The molecular mass of p53 is 53 KD. The p53 has the function of regulating the cell cycle, thus, it functions as preventing cancer, a tumor suppressor. The p53 plays an important role in apoptosis, inhibition of angiogenesis and genomic stability by activating DNA repair proteins, arresting cell growth though holding the cell cycle and initiating apoptosis. p53 becomes activated in response to DNA damage, osmotic shock, oxidative stress or other myriad stressors. Activated p53 activates the expression of several genes by binding DNA including p21.

References: Bioorg Med Chem. 2011 Mar 1; 19(5):1649-57; ACS Chem Neurosci. 2014 May 21; 5(5): 390–399.

Related CAS: 511296-88-1 (HBr); 2109248-93-1 (HCl)