Pifithrin-μ

Biological Activity

Pifithrin-μ inhibits p53 binding to mitochondria by reducing its affinity for antiapoptotic proteins Bcl-2 and Bcl-XL. Displays no effect on the transactivational or cell cycle checkpoint control function of p53. Potentially increases reprogramming efficiency of human somatic cells to induced pluripotent stem cells (iPSCs) by silencing p53. Pifithrin-μ reduces cell death induced by γ-radiation in vitro and protects mice from doses of radiation that cause lethal hematopoietic syndrome. Selectively inhibits heat shock protein 70 (HSP70) activity.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 2-phenylacetylenesulfonamide (PAS) induces p53-independent apoptotic killing of B-chronic lymphocytic leukemia (CLL) cells.
   Steele et al.
   Blood, 2009;114:1217
2. A small molecule inhibitor of inducible heat shock protein 70 (HSP70).
   Leu et al.
   Mol.Cell, 2009;36:15
3. Linking the p53 tumor suppressor pathway to somatic cell reprogramming.
   Kawamura et al.
   Nature, 2009;460:1140
4. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
   Strom et al.
   Nat.Chem.Biol., 2006;2:474

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