1. Metabolic Enzyme/Protease
  2. Proteasome
  3. Proteasome inhibitor IX

Proteasome inhibitor IX (Synonyms: PS-IX; AM114)

目录号: HY-107412 纯度: 98.53%
产品使用指南

Proteasome inhibitor IX (PS-IX; AM114) 是一种 Chalcone 衍生物,也是一种 20S 蛋白酶体 (20S proteasome) 的胰凝乳蛋白酶样活性抑制剂,IC50 值约为 1 μM。Proteasome inhibitor IX 具有 HCT116 p53+/+ 细胞生长抑制活性,IC50 值为 1.49 μM,具有有效的抗癌活性。

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Proteasome inhibitor IX Chemical Structure

Proteasome inhibitor IX Chemical Structure

CAS No. : 856849-35-9

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Description

Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity[1][2].

IC50 & Target

IC50: 1 μM (20S proteasome)[1]

In Vitro

Proteasome inhibitor IX (AM114; 0.1-10 µM; 14 days; HCT116 p53+/+ cells) treatment causes a loss of cell survival in the p53+/+ and p53-/- cells by approximately 70 and 20%, respectively at a concentration of 1 µM[1].
Proteasome inhibitor IX (AM114) exhibits potent activity against p53+/+ cells in colony formation assay, with an IC50 value of 0.6 µM[1].
Incubation of HCT116 p53+/+ cells with 1 µM Proteasome inhibitor IX (AM114) causes 28% of the cells to exhibit positive Annexin V staining at 48 h, and this fraction of dead cells increased to 76% at 72 h[1].
Proteasome inhibitor IX (AM114) treatment inhibits the chymotrypsin-like activity of the 20S proteasome in vitro, leading to a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells[1].

Molecular Weight

377.01

Formula

C₂₀H₂₁B₂NO₅

CAS No.

856849-35-9

SMILES

O=C(/C(CN(C)C/1)=C\C2=CC=C(B(O)O)C=C2)C1=C/C3=CC=C(B(O)O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (16.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6524 mL 13.2622 mL 26.5245 mL
5 mM 0.5305 mL 2.6524 mL 5.3049 mL
10 mM 0.2652 mL 1.3262 mL 2.6524 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: ≥ 0.62 mg/mL (1.64 mM); Clear solution

    此方案可获得 ≥ 0.62 mg/mL (1.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.2 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.62 mg/mL (1.64 mM); Clear solution

    此方案可获得 ≥ 0.62 mg/mL (1.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
References
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Keywords:

Proteasome inhibitor IXPS-IXAM114AM 114AM-114ProteasomeAnticancerboronicacidEGCGcytotoxicChalconep53chymotrypsin-like20SubiquitinatedInhibitorinhibitorinhibit

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产品名称:
Proteasome inhibitor IX
目录号:
HY-107412
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