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Cat. No. M2036

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Pifithrin-α Structure

Pifithrin hydrobromide; PFTα hydrobromide

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
50mg USD 320  USD320 In stock
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Biological Activity

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.

Product Citations
Chemical Information
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

[1] Dagher PC, et al. Am J Physiol Renal Physiol. The p53 inhibitor pifithrin-α can stimulate fibrosis in a rat model of ischemic acute kidney injury.

[2] Murphy PJ, et al. J Biol Chem. Pifithrin-alpha inhibits p53 signaling after interaction of the tumor suppressor protein with hsp90 and its nuclear translocation.

[3] Komarova EA, et al. J Biol Chem. p53 inhibitor pifithrin alpha can suppress heat shock and glucocorticoid signaling pathways.

[4] Komarov PG, et al. Science. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.

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Keywords: Pifithrin-α, Pifithrin hydrobromide; PFTα hydrobromide supplier, p53, inhibitors, activators

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