PI-1840|cas:1401223-22-0|西域试剂

PI-1840,99.11%

产品编号：Bellancom-12286| CAS NO：1401223-22-0| 分子式：C₂₂H₂₆N₄O₃| 分子量：394.47

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货号	价格	库存与货期
Bellancom-12286	￥1080.00	杭州北京（现货）
Bellancom-12286	￥3900.00	杭州北京（现货）
Bellancom-12286	￥7200.00	杭州北京（现货）

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PI-1840

产品介绍

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 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.

体外研究

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.

西域 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.

西域 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%.

体内研究

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

西域 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%.

体内研究

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

西域 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%.

性状

Solid

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 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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。