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Cat. No. M2036
Pifithrin-α Structure

Pifithrin hydrobromide; PFTα hydrobromide

Size Price Availability Quantity
5mg USD 54  USD60 In stock
10mg USD 81  USD90 In stock
50mg USD 288  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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 367.3
Formula C16H18N2OS.HBr
CAS Number 63208-82-2
Purity >99%
Solubility DMSO 57 mg/mL
Storage at -20°C

The p53 inhibitor pifithrin-α can stimulate fibrosis in a rat model of ischemic acute kidney injury.
Dagher PC, et al. Am J Physiol Renal Physiol. 2012 Jan 15;302(2):F284-91. PMID: 22049400.

Pifithrin-alpha inhibits p53 signaling after interaction of the tumor suppressor protein with hsp90 and its nuclear translocation.
Murphy PJ, et al. J Biol Chem. 2004 Jul 16;279(29):30195-201. PMID: 15145929.

p53 inhibitor pifithrin alpha can suppress heat shock and glucocorticoid signaling pathways.
Komarova EA, et al. J Biol Chem. 2003 May 2;278(18):15465-8. PMID: 12637507.

A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.
Komarov PG, et al. Science. 1999 Sep 10;285(5434):1733-7. PMID: 10481009.

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

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