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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別名: Pifithrin-α, p-nitro, cyclic is also known as p-nitro-Cyclic PFT-α.
アプリケーション: Pifithrin-α, p-nitro, cyclic is A cell-permeable p53 inhibitor that is more potent & has a longer half-life than Pifithrin-α.
CAS 番号: 60477-38-5
Purity: ≥95%
Molecular Weight: 299.35
Molecular Formula: C15H13N3O2S
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* 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.


参考文献

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).
保存方法 :
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)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
PubChem CID :
MDL Number :
MFCD05670249
SMILES :
C1CCC2=C(C1)N3C=C(N=C3S2)C4=CC=C(C=C4)[N+](=O)[O-]

Download SDS (MSDS)

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

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引用 1 to 1 of 1 合計

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

引用 1 to 1 of 1 合計
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