AM 114

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。

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10mg

￥1100.00

880.00

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￥3775.00

3020.00

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货号: ajci11820
CAS: 856849-35-9
别名: PS-IX; AM114
分子式: C20H21B2NO5
分子量: 377.01
纯度: >98%
溶解度: ≥ 16.65mg/mL in DMSO, ≥ 4.11 mg/mL in EtOH with ultrasonic
储存: Store at 4°C
库存: 现货

Background

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 IC₅₀ of 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 IC₅₀ of 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.