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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Alternate Names: Pifithrin-α, p-nitro, cyclic is also known as p-nitro-Cyclic PFT-α.
Application Pifithrin-α, p-nitro, cyclic is A cell-permeable p53 inhibitor that is more potent & has a longer half-life than Pifithrin-α.
CAS 등록번호: 60477-38-5
순도: ≥95%
분자량: 299.35
분자식: C15H13N3O2S
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
* 참조분석증명서대량의 측정 데이터(함수량포함).

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.


References

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
용해도 :
Soluble in DMSO (2.5 mg/ml), and ethanol (250 µg/ml).
저장 :
Store at -20° C
녹는점 :
212.44° C (Predicted)
비등점 :
499.66° C (Predicted)
밀도 :
1.53 g/cm3 (Predicted)
굴절률 :
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)
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
PubChem CID :
MDL Number :
MFCD05670249
SMILES :
C1CCC2=C(C1)N3C=C(N=C3S2)C4=CC=C(C=C4)[N+](=O)[O-]

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

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