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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备用名: Pifithrin-α, p-nitro, cyclic is also known as p-nitro-Cyclic PFT-α.
应用; Pifithrin-α, p-nitro, cyclic is A cell-permeable p53 inhibitor that is more potent & has a longer half-life than Pifithrin-α.
CAS号码: 60477-38-5
纯度: ≥95%
分子量: 299.35
分子式: C15H13N3O2S
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

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).

物理状态 :
Solid
溶解度 :
Soluble in DMSO (2.5 mg/ml), and ethanol (250 µg/ml).
保存 :
Store at -20° C
熔点 :
212.44° C (Predicted)
沸点 :
499.66° C (Predicted)
密度 :
1.53 g/cm3 (Predicted)
折射率 :
n20D 1.78 (Predicted)
IC50 :
Effective concentration required to protect mouse embryo cortical neurons against a DNA-damaging agent: EC5050 = 0.03 µM
pK值 :
pKb: 6.14 (Predicted)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
MDL 号码 :
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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