Pifithrin-α, p-nitro, cyclic CAS: 60477-38-5
MF: C15H13N3O2S
MW: 299.35

Pifithrin-α, p-nitro, cyclic (CAS 60477-38-5)

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Alternativa namn: Pifithrin-α, p-nitro, cyclic is also known as p-nitro-Cyclic PFT-α.
Ansökan Pifithrin-α, p-nitro, cyclic is A cell-permeable p53 inhibitor that is more potent & has a longer half-life than Pifithrin-α.
CAS Nr: 60477-38-5
Renhet: ≥95%
Molekylvikt: 299.35
Molekylär formel: C15H13N3O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

Pifithrin-α, p-Nitro, Cyclic is a cell-permeable p53 inhibitor that exhibits 10-fold higher potency (ED50 = 30 nM in protecting etoposide-induced cortical neuron death) and 50% longer half-life (t1/2 = 6h in neuron culture medium at 37° C) than Pifithrin-α. Pifithrin-α, p-nitro, cyclic behaves p53-dependently but does not block p53 phosphorylation on Ser15 in reponse to etoposide treatment. Pifithrin-α, p-nitro, cyclic will block p53 posttranscriptional activity, however. Pifithrin-α, p-nitro, cyclic is more stable than the parent compound. Pifithrin-α, p-nitro, cyclic is not active in vivo.


Konferenser

1. Komarov, P.G., Komarova, E.A., Kondratov, R.V., et al.A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 285(5434), 1733-1737 (1999).
2. Walton, M.I., Wilson, S.C., Hardcastle, I.R., et al.An evaluation of the ability of pifithrin-α and -β to inhibit p53 function in two wild-type p53 human tumor cell lines. Mol. Cancer Ther. 4(9), 1369-1377 (2005).
3. Pietrancosta, N., Moumen, A., Dono, R., et al.Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: Discovery of a highly potent in vivo inhibitor and its action mechanism. Journal of Medicinal Chemistry 49(12), 3645-3652 (2006).

Physical State :
Solid
Solubility :
Soluble in DMSO (2.5 mg/ml), and ethanol (250 µg/ml).
LAGRING :
Store at -20° C
Melting Point :
212.44° C (Predicted)
Boiling Point :
499.66° C (Predicted)
Density :
1.53 g/cm3 (Predicted)
Refractive Index :
n20D 1.78 (Predicted)
IC50 :
Effective concentration required to protect mouse embryo cortical neurons against a DNA-damaging agent: EC5050 = 0.03 µM
pK Values :
pKb: 6.14 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
MDL Number :
MFCD05670249
SMILES :
C1CCC2=C(C1)N3C=C(N=C3S2)C4=CC=C(C=C4)[N+](=O)[O-]

Download SDS (MSDS)

Certificate of Analysis

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Pifithrin-α, p-nitro, cyclic (CAS 60477-38-5)  Produkt Citat

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PMID: # 31236885  Bull Exp Biol Med. 201-206.

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