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: 1 μM (20S proteasome)^[1]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

377.01

C₂₀H₂₁B₂NO₅

856849-35-9

Room temperature in continental US; may vary elsewhere.

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

In Vitro: 

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

*

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

• [1]. Geetha Achanta , et al. A Boronic-Chalcone Derivative Exhibits Potent Anticancer Activity Through Inhibition of the Proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33.

  [2]. Encouse B Golden, et al. Green Tea Polyphenols Block the Anticancer Effects of Bortezomib and Other Boronic Acid-Based Proteasome Inhibitors. Blood. 2009 Jun 4;113(23):5927-37.