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PI-1840
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PI-1840图片
CAS NO:1401223-22-0

PI-1840 是一种有效的选择性凝乳胰蛋白酶样 (CT-L) 抑制剂,其IC50值为 27 nM。PI-1840 抑制细胞增殖, 将细胞周期阻滞在 G2/M 期。PI-1840 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。PI-1840 诱导蛋白酶体底物 p27、Bax 和 IκB-α 的积累。
生物活性

PI-1840 is a potent and selectivechymotrypsin-like (CT-L)inhibitor for with anIC50value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 inducesapoptosisand inducesautophagy. PI-1840 induces the accumulation ofproteasomesubstrates p27,Bax, and IκB-α[1][2].

体外研究
(In Vitro)

PI-1840 (5-60 μM; 24 and 48 h) inhibits the proliferation of MG-63 and U2-OS cells[1].
PI-1840 (40 μM (U2-OS cells) and 60 μM (MG-63 cells); 24 and 48 h) induces cell cycle arrest at the G2/M phase[1].
PI-1840 (15-60 μM (MG-63 cells), 10-40 μM (U2-OS cells); 48 h) induces apoptosis through NF-κB pathway in MG-63 and U2-OS cells. PI-1840 induces autophagy in MG-63 and U2-OS cells[1].

Cell Viability Assay[1]

Cell Line:MG-63 and U2-OS cells
Concentration:5, 10, 20, 40, 80, and 160 μM
Incubation Time:24 and 48 hours
Result:Inhibited cell growth in a dose-dependent manner with IC50values of 108.40 μM (MG-63, 24 h), 59.58 μM (MG-63, 48 h), 86.43 μM (U2-OS, 24 h), and 38.83 μM (U2-OS, 48 h), respectively.

Apoptosis Analysis[1]

Cell Line:MG-63 and U2-OS cells
Concentration:15, 30, and 60 μM (MG-63 cells), 10, 20, and 40 μM (U2-OS cells)
Incubation Time:48 hours
Result:Increased the apoptotic rates of the two cell lines in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line:MG-63 and U2-OS cells
Concentration:40 μM (U2-OS cells) and 60 μM (MG-63 cells)
Incubation Time:24 and 48 hours
Result:Increased in the G2/M phase cell population.

Western Blot Analysis[1]

Cell Line:MG-63 and U2-OS cells
Concentration:40 μM (U2-OS cells) and 60 μM (MG-63 cells)
Incubation Time:24 and 48 hours
Result:Increased the cell cycle regulation-associated proteins about p21, p27 and WEE1.

Western Blot Analysis[1]

Cell Line:MG-63 and U2-OS cells
Concentration:15, 30, and 60 μM (MG-63 cells), 10, 20, and 40 μM (U2-OS cells)
Incubation Time:48 hours
Result:Increased the ratio of the expression level of (p-IκBα/control)/(IκBα/control), and decreased the ratio of (p-p65/control)/(p65/control).
Decreased the expression level of Bcl-2 and the mitochondrial proteins Cyto c.
Increased the expression levels of Bax, and the ratios of (cleaved caspase-3/caspase-3, cleaved PARP/PARP, cleaved caspase-8/caspase-8 and cleaved caspase-9/caspase-9.
Increased the ratio of LC3 II to LC 3 I, and the expression level of Beclin1.
体内研究
(In Vivo)

PI-1840 (150 mg/kg; i.p.; daily, for 14 d) inhibits the growth of human breast tumor xenografts in nude mice[2].

Animal Model:Female nude mice with MDA-MB-231 xenografts[2]
Dosage:150 mg/kg
Administration:Intraperitoneal injection; daily, for 14 days
Result:Inhibited the growth of MDA-MB-231 tumor xenografts by 76%.
分子量

394.47

性状

Solid

Formula

C22H26N4O3

CAS 号

1401223-22-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(253.50 mM;Need ultrasonic)

H2O : 0.1 mg/mL(0.25 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5350 mL12.6752 mL25.3505 mL
5 mM0.5070 mL2.5350 mL5.0701 mL
10 mM0.2535 mL1.2675 mL2.5350 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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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