Pifithrin-mu An inhibitor of p53 activity and HSP 70 activity

Pifithrin-μ (CAS 64984-31-2)

Pifithrin-andmu, CAS 64984-31-2 is rated 5.0 out of 5 by 1.
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Synonym: 2-Phenylacetylenesulfonamide; NSC 303580
Application: An inhibitor of p53 activity and HSP 70 activity
CAS Number: 64984-31-2
Purity: ≥98%
Molecular Weight: 181.2
Molecular Formula: C8H7NO2S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Pifithrin-μ is a cell-permeable sulfonamide inhibitor of p53 binding and an anti-apoptotic. Direct inhibition of p53 binding to mitochondria as well as to Bcl-xL and Bcl-2 proteins by Pifithrin-μ has been observed. Pifithrin-μ selectively inhibits p53 translocation to mitochondria without affecting the transactivation function of p53. Pifithrin-μ has been shown to reduce γ-radiation induced cell death in vitro. Unlike pifithrin-α (sc-45050), pifithrin-μ targets only the mitochondrial branch of the p53 pathway without affecting the important transcriptional functions of p53. Pifithrin-μ selectively inhibits HSP 70 (heat shock protein 70) activity.


References

1. Strom, Evguenia., et al., 2006. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nature chemical biology. 2(9): 474-9. PMID: 16862141
2. Vaseva, Angelina V., et al., 2009. The transcription-independent mitochondrial p53 program is a major contributor to nutlin-induced apoptosis in tumor cells. Cell cycle (Georgetown, Tex.). 8(11): 1711-9. PMID: 19411846
3. Subramanian, S V., et al., 2009. Do burdens of underweight and overweight coexist among lower socioeconomic groups in India? The American journal of clinical nutrition. 90(2): 369-76. PMID: 19515733
4. Drakos, E., et al., 2009. The therapeutic potential of p53 reactivation by nutlin-3a in ALK+ anaplastic large cell lymphoma with wild-type or mutated p53. Leukemia. 23(12): 2290-9. PMID: 19741726
5. Hagn, Franz., et al., 2010. BclxL changes conformation upon binding to wild-type but not mutant p53 DNA binding domain. The Journal of biological chemistry. 285(5): 3439-50. PMID: 19955567
6. Xu, Xia., et al., . Enhancement of cell recovery for dissociated human embryonic stem cells after cryopreservation. Biotechnology progress. 26(3): 781-8. PMID: 20014103

Physical State :
Solid
Solubility :
Soluble in DMSO (>10 mg/mL), water (<2 mg/mL), and ethanol (100 mM).
Storage :
Store at 4° C
Melting Point :
136-138° C
Boiling Point :
351.70° C at 760 mmHg (Predicted)
Density :
1.40 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
pK Values :
pKa: 7.96 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
327653
MDL Number :
MFCD00181531
SMILES :
C1=CC=C(C=C1)C#CS(=O)(=O)N

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Certificate of Analysis

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Pifithrin-mu  Product Citations

See how others have used Pifithrin-mu. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 26884717  Yu, W. et al. 2016. Int. J. Biol. Sci. 12: 198-209.

PMID: # 26703711  Claus, C. et al. 2015. Viruses. 7: 6108-26.

PMID: # 24244355  Sekihara, K. et al. 2013. PLoS ONE. 8: e78772.

PMID: # 19955567  Hagn, F. et al. 2010. J. Biol. Chem. 285: 3439-3450.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Hagn Hagn, F. et al. (PubMed 19955567) presented the first structural data of Pifithrin- (NSC 303580), an inhibitor of p53 that blocks its interaction with BclxL and Bcl-2. They found that Pifithrin- inhibits this interaction by binding to both sides of the p53-BclxL protein complex. -SCBT Publication Review
Date published: 2015-04-07
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