1401223-22-0|PI-1840，≥98%|Medlife为MCE，Selleck，麦克林，阿拉丁试剂，罗恩试剂，Sigma，安耐吉试剂，泰坦等同类产品品牌，上海现货，性价比高

您当前的位置：

PI-1840

胰凝乳蛋白酶样(CT-L)抑制剂，PI-1840是蛋白酶体chymotrypsin-like (CT-L)高效选择性性抑制剂，IC50值为27nM。

目录号: PC16239 纯度: ≥98%

CAS No. :1401223-22-0

商品编号	规格	价格	会员价	是否有货	数量
PC16239-10mg	10mg	¥1136.80	请登录
PC16239-50mg	50mg	¥3998.40	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称

PI-1840

中文别名

N-异丙基-2-(4-丙基苯氧基)-N-((3-(吡啶-3-基)-1,2,4-噁二唑-5-基)甲基)乙酰胺;PI-1840

英文名称

PI-1840

英文别名

PI 1840;N-isopropyl-2-(4-propylphenoxy)-N-(((3-pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide;N-Isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide;PI-1840

Cas No.

1401223-22-0

分子式

C₂₂H₂₆N₄O₃

分子量

394.47

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC₅₀ value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.

性状

Solid

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.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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 IC₅₀ values 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

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

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

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

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Kazi A, et, al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014 Apr 25;289(17):11906-11915. [Information]

[2]. Chen Y, et, al. Non covalent proteasome inhibitor PI 1840 induces apoptosis and autophagy in osteosarcoma cells. Oncol Rep. 2019 May;41(5):2803-2817. [Information]

溶解度数据

体外研究:

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

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

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5350 mL	12.6752 mL	25.3505 mL
5 mM	0.5070 mL	2.5350 mL	5.0701 mL
10 mM	0.2535 mL	1.2675 mL	2.5350 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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。

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation