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Description: Pifithrin-alpha ((PFTalpha) is a novel and potent inhibitor of p53, acting by inhibiting p53 protein transcription and p53-dependent transactivation of p53-responsive genes. It also acts as an aryl hydrocarbon receptor (AhR) agonist. Pifithrin-alpha was firstly found to block the activation of p53-responsive lacZ in ConA cells and reduce activation of endogenous cellular p53-responsive genes. Pifithrin-alpha can also induce cell cycle arrest and growth arrest of embryonic stem cells. Treatment of Pifithrin-alpha significantly downregulates the protein lever of Nanog (a pluripotency marker). It is proved that the inhibition of p53 activity caused by Pifithrin-alpha has no effect on ES cell viability.
Reference: Science. 1999 Sep 10; 285(5434):1733-7.
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