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AM 114
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。
AM 114图片
CAS NO:856849-35-9
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
AM 114 (PS-IX; AM114) 是查尔酮衍生物和 20S 蛋白酶体抑制剂的糜蛋白酶样活性,IC50 值为 ~1 μM. AM 114 表现出 HCT116 p53+/+ 细胞生长抑制活性,IC50 值为 1.49 μM. AM 114 具有强大的抗癌活性。
Cas No.856849-35-9
别名PS-IX; AM114
化学名[4-[(Z)-[(5Z)-5-[(4-boronophenyl)methylidene]-1-methyl-4-oxopiperidin-3-ylidene]methyl]phenyl]boronic acid
Canonical SMILESB(C1=CC=C(C=C1)C=C2CN(CC(=CC3=CC=C(C=C3)B(O)O)C2=O)C)(O)O
分子式C20H21B2NO5
分子量377.01
溶解度≥ 16.65mg/mL in DMSO, ≥ 4.11 mg/mL in EtOH with ultrasonic
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50of approximately 1 μM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. AM 114 also exerts anti-cancer activity against cancer cells, which potently inhibits the growth of human colon cancer HCT116 cells with values of IC50of 1.5 μM and 0.6 μM in MTT and colony formation assays respectively.

Reference

[1].Achanta G, Modzelewska A, Feng L, Khan SR, Huang P. A boronic-chalcone derivative exhibits potent anticancer activity through inhibition of the proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33. Epub 2006 Apr 24.