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Pifithrin-α (PFTalpha) is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. 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 enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation without an increase in cancer incidence. Pifithrin-α can also protect cells from DNA damage-induced apoptosis by a p53-independent mechanism that might involve cyclin D1. In addition to p53, PFTalpha can suppress heat shock and glucocorticoid receptor signaling but has no effect on nuclear factor-kappaB signaling. Pifithrin-α (PFTalpha) reduces activation of heat shock transcription factor (HSF1) and increases cell sensitivity to heat. Moreover, Pifithrin-α reduces activation of glucocorticoid receptor and rescues mouse thymocytes in vitro and in vivo from apoptotic death after dexamethasone treatment.
Sci Total Environ. 2023 Dec;30:913:169730.
Selenium deficiency exacerbated Bisphenol A-induced intestinal toxicity in chickens: Apoptosis and cell cycle arrest mediated by ROS/P53
Pifithrin-α purchased from AbMole
Adv Sci (Weinh). 2022 Nov 22;10(1):e2204463.
Genetic and Pharmacological Inhibition of Astrocytic Mysm1 Alleviates Depressive-Like Disorders by Promoting ATP Production
Pifithrin-α purchased from AbMole
Ecotoxicol Environ Saf. 2022 Jun 1;237:113564.
Environmental BPDE induced human trophoblast cell apoptosis by up-regulating lnc-HZ01/p53 positive feedback loop
Pifithrin-α purchased from AbMole
| Molecular Weight | 367.3 |
| Formula | C16H18N2OS.HBr |
| CAS Number | 63208-82-2 |
| Solubility (25°C) | DMSO 57 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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Products are for research use only. Not for human use. We do not sell to patients.
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