An inhibitor of p53-mediated apoptosis

Pifithrin-μ – 5 mg

Brand:
Cayman
CAS:
64984-31-2
Storage:
-20
UN-No:
Non-Hazardous - /

In addition to its transactivational functions, p53 mediates apoptosis by binding with the anti-apoptotic proteins Bcl-xL and Bcl-2 at the mitochondrial surface.{19632,19633} Pifithrin-μ (PFT-μ) is an inhibitor of p53-mediated apoptosis, preventing p53 binding to Bcl-xL and Bcl-2 at the mitochondria without affecting p53 transactivational activities{19632} In vitro, PFT-μ binds both p53 (Kd = 0.82 mM) and Bcl-xL (Kd = 0.80 mM).{19630} PFT-μ reduces p53-mediated apoptosis induced by γ-radiation in mouse thymocytes in vitro and protects mice from doses of radiation that cause lethal hematopoietic syndrome. At 25 μM, PFT-μ reduces apoptosis triggered by nutlin-3, which inhibits MDM2/p53 binding and potentiates p53-mediated growth arrest and apoptosis.{19633} PFT-μ also interacts selectively with heat shock protein 70 (Hsp70), leading to disruption of the association between Hsp70 and many of its co-chaperones and substrate proteins.{19631}  

 

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SKU: 10748 - 5 mg Category:

Description

An inhibitor of p53-mediated apoptosis, preventing p53 binding at the mitochondrial surface without affecting p53 transactivational activities; at 25 μM, pifithrin-μ reduces p53-mediated apoptosis triggered by nutlin; also interacts selectively with Hsp70, disrupting its association with many substrate proteins

Formal name: 2-phenyl-ethynesulfonamide

Synonyms:  2-Phenylethynesulfonamide|PFT-μ

Molecular weight: 181.2

CAS: 64984-31-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cell Biology|Cellular Chaperones||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Innate Immunity

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