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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 181.21. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||5.52 mL||27.59 mL||55.18 mL|
|5 mM||1.1 mL||5.52 mL||11.04 mL|
|10 mM||0.55 mL||2.76 mL||5.52 mL|
|50 mM||0.11 mL||0.55 mL||1.1 mL|
References are publications that support the biological activity of the product.
Strom et al (2006) Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nat.Chem.Biol. 2 474 PMID: 16862141
Leu et al (2009) A small molecule inhibitor of inducible heat shock protein 70 (HSP70). Mol.Cell 36 15 PMID: 19818706
Kawamura et al (2009) Linking the p53 tumor suppressor pathway to somatic cell reprogramming. Nature 460 1140 PMID: 19668186
Steele et al (2009) 2-phenylacetylenesulfonamide (PAS) induces p53-independent apoptotic killing of B-chronic lymphocytic leukemia (CLL) cells. Blood 114 1217 PMID: 19515722
If you know of a relevant reference for Pifithrin-μ, please let us know.
Keywords: Pifithrin-mu, Pifithrin-mu supplier, inhibitors, inhibits, p53-mitochondrial, binding, Transcription, Factors, MDM2, p14ARF, Pifithrin-mu, NSC303580, NSC, 303580, p53, Stem, Cell, Reprogramming, Hsp70, 2653, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Pifithrin-μ include:
Li et al (2018) Zinc deficiency causes neural tube defects through attenuation of p53 ubiquitylation. Development 145 PMID: 30545932
Kojima et al (2010) The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. Mol Cancer Ther 9 2545 PMID: 20736344
Blatzer et al (2015) Blocking Hsp70 Enhances the Efficiency of amphote. B Treatment against Resistant Aspergillus terreus Strains. Antimicrob Agents Chemother 59 3778 PMID: 25870060
Wang et al (2013) Active Constituents from Liriope platyphylla Root against Cancer Growth In Vitro. PLoS One 2013 857929 PMID: 23762164
Nemade et al (2018) Cell death mechanisms of the anti-cancer drug EPEG on human cardiomyocytes isolated from pluripotent stem cells. Arch Toxicol 92 1507 PMID: 29397400
Xia et al (2014) EZH2 silencing with RNA interference induces G2/M arrest in human lung cancer cells in vitro. Biomed Res Int 2014 348728 PMID: 24745014
Do you know of a great paper that uses Pifithrin-μ from Tocris? Please let us know.
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Pifithrin-µ were dissolved in DMSO and used at a final concentration of 50 µM for pifithrin-µ according to previous studies in which 10-50 µM pifithrin-µ were employed.
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This product guide provides a review of the cell cycle and DNA damage research area and lists over 170 products, including research tools for:
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.