Pifithrin-α,p-Nitro,Cyclic

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CAS NO:

60477-38-5

PFN-α

Pifithrin-α, p-Nitro, Cyclic (PFN-α)，是细胞通透性的p53抑制剂。Pifithrin-α, p-Nitro, Cyclic 对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级 (ED₅₀=30 nM)。Pifithrin-α, p-Nitro, Cyclic 也作为 p53 转录后活性抑制剂。Pifithrin-α, p-Nitro, Cyclic 不阻止 p53 上的 S15 残基磷酸化。

生物活性

Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-formp53inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED₅₀=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue^[1]^[2].

体外研究
(In Vitro)

Pifithrin-α, p-Nitro, Cyclic (PFN-α) efficiently blocks p53-triggered cell death and p21/WAF1 expression in cortical neurons exposed to etoposide at concentrations one order magnitude lower than that in PFT-α^[1].

体内研究
(In Vivo)

Intraocular injection of pifithrin-α slightly increases survival of retinal ganglion cell (RGC) at the concentration of 6 μM but not at 0.06 μM. Pifithrin-α, p-Nitro, Cyclic (PFN-α) is not effective in vivo, even at 6 μM^[1].
Pifithrin-α, p-Nitro, Cyclic shows the half-life (t_1/2) of 6 hours (when incubated in biological conditions)^[1].

分子量

299.35

性状

Solid

Formula

C₁₅H₁₃N₃O₂S

CAS 号

60477-38-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMF : 12.5 mg/mL(41.76 mM;Need ultrasonic)

DMSO : 5 mg/mL(16.70 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.3406 mL	16.7029 mL	33.4057 mL
5 mM	0.6681 mL	3.3406 mL	6.6811 mL
10 mM	0.3341 mL	1.6703 mL	3.3406 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。