2-(2-Amino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-ium-3-yl)-1-(4-methylphenyl)ethanone bromide

개요Pifithrin-α is an inactivator of p53 that blocks p53-dependent transcriptional activation and apoptosis. It prevents p53-mediated apoptosis induced by cytotoxic compounds in C8 cells at 10 μM and in human umbilical vein endothelial cells at 30 μM. Pifithrin-α can also protect cells from DNA damage-induced apoptosis by a p53-independent mechanism that might involve cyclin D1.

용도Pifithrin-α has been used:to study the effect of specific p53 inhibitor on p53-upregulated modulator of apoptosis (PUMA) expression after transient global cerebral ischemia (tGCI)as p53 inhibitor to treat PA1 cellsas a tumor protein p53 (TRP53) inhibitor, to treat mouse lung epithelial-12 (MLE-12) cells

일반 설명A cell-permeable chemical inhibitor of p53. Reversibly inhibits p53-dependent transactivation of p53-responsive genes and reversibly blocks p53-mediated apoptosis. Inhibits p53-dependent growth arrest of human diploid fibroblasts in response to DNA damage but has no effect on p53-deficient fibroblasts. Protects normal tissues from the deleterious side effects of chemotherapy. Has been reported to protect neurons against β-amyloid peptide and glutamate-induced apoptosis.